Journal articles: 'Synthesis of chalcones'

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Chen, Jie, Chen-Fu Liu, and Guo-Wu Rao. "Progress in the Synthesis, Angiogenesis Activity and Mechanism of Chalcone Derivatives." Mini-Reviews in Organic Chemistry 17, no. 7 (October 9, 2020): 814–27. http://dx.doi.org/10.2174/1570193x17666191223161941.

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Cancer is a common disease that poses a serious threat to human health. Angiogenesis is essential for the growth and metabolism of tumors, providing oxygen and nutrition for the growth of cells and tissues. However, angiogenesis of tumors depends on the stimulation of growth factors. Vascular Endothelial Growth Factor (VEGFR) is the most unique factor. Therefore, VEGF/VEGFR targeting anticancer drugs are playing an increasingly significant role in clinical trials. In addition, it has been proved that chalcone, the precursor of natural flavonoids, has potential anti-tumor activity, especially anti-angiogenesis activity. This review summarizes the reports about the anti-angiogenesis of chalcone derivatives. Based on the chalcone skeleton, it is divided into substituted chalcones and modified chalcones. The anti-angiogenesis activities of natural or synthetic chalcones, benzene ring modified or connecting bridge modified chalcones are described in this review.

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K. Saini, K. Rajendra, S. Amit Choudhary, Yogesh C. Joshi, and P. Joshi. "Solvent Free Synthesis of Chalcones and their Antibacterial Activities." E-Journal of Chemistry 2, no. 4 (2005): 224–27. http://dx.doi.org/10.1155/2005/294094.

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The solvent free synthesis of six chalcones was carried out by grinding the piperanal and the acetophenone (unsubstituted, 4-methyl, 4-methoxy, 4-bromo, 4-nitro, 3-chloro) in the presence of solid sodium hydroxide with a mortar and pestle. In general, the chalcones were obtained in high yield and high purity. Minor quantities of Ketol and Michael addition product were easily removed by recrystallization. The result indicates a correlation between the success of the solvent-free synthesis and melting point of the chalcone. Chalcone with relatively high melting points (higher than 80°C) were obtained in high yields. The two chalcones that could not be produced in good yields were having relatively low melting points. They have been screened for their antibacterial activity against Gram positive and Gram negative bacteria.

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Jasim, Hiba A., Lutfun Nahar, Mohammad A. Jasim, Sharon A. Moore, Kenneth J. Ritchie, and Satyajit D. Sarker. "Chalcones: Synthetic Chemistry Follows Where Nature Leads." Biomolecules 11, no. 8 (August 13, 2021): 1203. http://dx.doi.org/10.3390/biom11081203.

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Chalcones belong to the flavonoid class of phenolic compounds. They form one of the largest groups of bioactive natural products. The potential anticancer, anti-inflammatory, antimicrobial, antioxidant, and antiparasitic properties of naturally occurring chalcones, and their unique chemical structural features inspired the synthesis of numerous chalcone derivatives. In fact, structural features of chalcones are easy to construct from simple aromatic compounds, and it is convenient to perform structural modifications to generate functionalized chalcone derivatives. Many of these synthetic analogs were shown to possess similar bioactivities as their natural counterparts, but often with an enhanced potency and reduced toxicity. This review article aims to demonstrate how bioinspired synthesis of chalcone derivatives can potentially introduce a new chemical space for exploitation for new drug discovery, justifying the title of this article. However, the focus remains on critical appraisal of synthesized chalcones and their derivatives for their bioactivities, linking to their interactions at the biomolecular level where appropriate, and revealing their possible mechanisms of action.

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Tantawy, Mohamed A., Farid M. Sroor, Magda F. Mohamed, Mostafa E. El-Naggar, Fatma M. Saleh, Hamdi M. Hassaneen, and Ismail A. Abdelhamid. "Molecular Docking Study, Cytotoxicity, Cell Cycle Arrest and Apoptotic Induction of Novel Chalcones Incorporating Thiadiazolyl Isoquinoline in Cervical Cancer." Anti-Cancer Agents in Medicinal Chemistry 20, no. 1 (April 10, 2020): 70–83. http://dx.doi.org/10.2174/1871520619666191024121116.

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Background: Chalcones are naturally occurring compounds found in various plant species which are widely used for the traditional popular treatments. Chalcones are distinguished secondary metabolites that are reported to display diverse biological activities such as antiviral, antiplatelet, anti-inflammatory, anticancer, antibacterial and antioxidant agents. The presence of a,ß-unsaturated carbonyl group in chalcones is assumed to be responsible for their bioactivity. In addition, heterocyclic compounds having nitrogen such as isoquinolines are of considerable interest as they constitute the core structural element of many alkaloids that have enormous pharmacological activities. Objective: The objective of this study is the synthesis and biological activity of novel chalcones incorporating thiadiazolyl isoquinoline as potential anticancer candidates. Different genetic tools were used in an attempt to know the mechanism of action of this compound against breast cancer. Methods: An efficient one pot synthesis of novel chalcones incorporating thiadiazolyl isoquinoline has been developed. The cytotoxic activity of the novel synthesized compounds was performed against four different kinds of cancer cell lines. Results: Among all the tested derivatives, chalcone 3 has the best cytotoxic profile against A549, MCF7, and HeLa cell lines, with IC50s (66.1, 51.3, and 85.1μM, respectively). Molecular docking studies for chalcone 3 revealed that CDK2, and EGFRTK domains have strong binding affinities toward the novel chalcone 3, while tubulin-colchicine-ustiloxin, and VEGFRTK domains illustrated moderate mode of binding. Conclusion: We have developed an efficient method for the synthesis of novel chalcones incorporating thiadiazolyl isoquinoline. All compounds showed better cytotoxicity results against four kinds of cancer cell lines (A549, MCF7, HCT116, and HELA cells). The results depicted that chalcone 3 has a high and promising cytotoxic effect against HELA cell line and the mechanism of cytotoxicity was widely studied through different theoretical and experimental tools. Thus, the newly synthesized derivative 3 can be utilized as a novel chemotherapeutic compound for cervical carcinoma.

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Farooq, Saba, and Zainab Ngaini. "Recent Synthetic Methodologies for Chalcone Synthesis (2013-2018)." Current Organocatalysis 6, no. 3 (September 5, 2019): 184–92. http://dx.doi.org/10.2174/2213337206666190306155140.

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An up-to-date short review of the chalcone methodologies is presented, which is the most interesting and beneficial for choosing the desired protocol to synthesize suitable derivatives of chalcones. Chalcones are fluorescent, stable compounds which contribute to the synthesis of various pharmacologically important heterocyclic structure-based derivatives. Chalcone has displayed a remarkable curative efficiency to cure several diseases. Several schemes and methodologies have been reported for employing different catalysts and reagents. The development of improved methodologies of α, β-unsaturated carbonyl compounds is still on going. In this review, synthetic methodologies and their recent modification in designing new methods with efficient, economical, eco-friendly and high yield are discussed.

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López, Génesis, Marco Mellado, Enrique Werner, Bastián Said, Patricio Godoy, Nelson Caro, Ximena Besoain, Iván Montenegro, and Alejandro Madrid. "Sonochemical Synthesis of 2’-Hydroxy-Chalcone Derivatives with Potential Anti-Oomycete Activity." Antibiotics 9, no. 9 (September 4, 2020): 576. http://dx.doi.org/10.3390/antibiotics9090576.

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This work reports on the synthesis of eight new 2′-hydroxy-chalcones with potential anti-phytopathogenic applications in agroindustry, AMONG others, via Claisen–Schmidt condensation and ultrasound assisted reaction. Assays showed three chalcones with allyl moieties strongly inhibited growth of phytopathogenic oomycete Phytophthora infestans; moreover, compound 8a had a half maximal effective concentration (EC50) value (32.5 µg/mL) similar to that of metalaxyl (28.6 µg/mL). A software-aided quantitative structure–activity relationship (QSAR) analysis of the whole series suggests that the structural features of these new chalcones—namely, the fluoride, hydroxyl, and amine groups over the carbon 3′ of the chalcone skeleton—increase anti-oomycete activity.

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Wijayanti, Lucia Wiwid, Respati Tri Swasono, Wonkoo Lee, and Jumina Jumina. "Synthesis and Evaluation of Chalcone Derivatives as Novel Sunscreen Agent." Molecules 26, no. 9 (May 4, 2021): 2698. http://dx.doi.org/10.3390/molecules26092698.

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Ultraviolet (UV) irradiation is a serious problem for skin health thus the interest in the research to develop sunscreen agent has been increasing. Chalcone is a promising compound to be developed as its chromophore absorbs in the UV region. Therefore, in the present work, we synthesized eight chalcone derivatives through Claisen–Schmidt condensation at room temperature. The evaluation of the optical properties of each chalcone derivatives in the UV region was conducted through spectroscopic and computational studies. The synthesized chalcones were obtained in good yields and they were active in the UV region. The results revealed that more methoxy substituents to chalcone leads toward red shift. All chalcone derivatives have high molar absorptivity value (21,000–56,000) demonstrating that they have the potential to be used as the sunscreen agent. The cytotoxicity assay showed that chalcone derivatives were demonstrating low toxicity toward normal human fibroblast cell, which is remarkable. Therefore, we concluded that the synthesized chalcones in this work were potential to be developed as novel sunscreen agents in real application.

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Ouyang, Yang, Juanjuan Li, Xinyue Chen, Xiaoyu Fu, Si Sun, and Qi Wu. "Chalcone Derivatives: Role in Anticancer Therapy." Biomolecules 11, no. 6 (June 16, 2021): 894. http://dx.doi.org/10.3390/biom11060894.

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Chalcones (1,3-diaryl-2-propen-1-ones) are precursors for flavonoids and isoflavonoids, which are common simple chemical scaffolds found in many naturally occurring compounds. Many chalcone derivatives were also prepared due to their convenient synthesis. Chalcones as weandhetic analogues have attracted much interest due to their broad biological activities with clinical potentials against various diseases, particularly for antitumor activity. The chalcone family has demonstrated potential in vitro and in vivo activity against cancers via multiple mechanisms, including cell cycle disruption, autophagy regulation, apoptosis induction, and immunomodulatory and inflammatory mediators. It represents a promising strategy to develop chalcones as novel anticancer agents. In addition, the combination of chalcones and other therapies is expected to be an effective way to improve anticancer therapeutic efficacy. However, despite the encouraging results for their response to cancers observed in clinical studies, a full description of toxicity is required for their clinical use as safe drugs for the treatment of cancer. In this review, we will summarize the recent advances of the chalcone family as potential anticancer agents and the mechanisms of action. Besides, future applications and scope of the chalcone family toward the treatment and prevention of cancer are brought out.

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B, Ravindar, Srinivasa Murthy M, and Afzal Basha Shaik. "DESIGN, FACILE SYNTHESIS, AND BIOLOGICAL EVALUATION OF NOVEL 1,3-THIAZINE DERIVATIVES AS POTENTIAL ANTICONVULSANT AGENTS." Asian Journal of Pharmaceutical and Clinical Research 9, no. 5 (September 1, 2016): 272. http://dx.doi.org/10.22159/ajpcr.2016.v9i5.13676.

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ABSTRACTObjective: Chalcones and their heterocyclic analogs represent an important class of small molecules having anticonvulsant activities. Therefore, inthis study, the synthesis and anticonvulsant activity of some new chalcones and 1,3-thiazines were described.Methods: The reaction of 1-acetylnaphthalene with substituted aromatic aldehydes in the presence of aq. NaOH afforded corresponding chalconeswhich upon further cyclization with thiourea resulted in 1,3-thiazine derivatives. The newly synthesized compounds were tested for anticonvulsantactivity by pentylenetetrazole-induced seizures method using diazepam as standard.Results: Most of the compounds showed good anticonvulsant activity but is less than diazepam. 1,3-thiazines were more potent than chalconesand among them, compound P4 containing 4-fluorophenyl substituents on the thiazine moiety was more potent as it has prolonged the onset ofconvulsions by 155.2 seconds.Conclusion: We described the synthesis and anticonvulsant activity of novel chalcones and 1,3-thiazine derivatives. 1,3-thiazines are more activeanticonvulsant agents than chalcones and in particular compounds with electron withdrawing substituents.Keywords: Chalcone, 1,3-thiazine, Pentylenetetrazole.

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Coşkun, Demet, Suat Tekin, Süleyman Sandal, and Mehmet Fatih Coşkun. "Synthesis, Characterization, and Anticancer Activity of New Benzofuran Substituted Chalcones." Journal of Chemistry 2016 (2016): 1–8. http://dx.doi.org/10.1155/2016/7678486.

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Benzofuran derivatives are of great interest in medicinal chemistry and have drawn considerable attention due to their diverse pharmacological profiles including anticancer activity. Similarly, chalcones, which are common substructures of numerous natural products belonging to the flavonoid class, feature strong anticancer properties. A novel series of chalcones, 3-aryl-1-(5-bromo-1-benzofuran-2-yl)-2-propanones propenones (3a–f), were designed, synthesized, and characterized.In vitroantitumor activities of the newly synthesized (3a–f) and previously synthesized (3g–j) chalcone compounds were determined by using human breast (MCF-7) and prostate (PC-3) cancer cell lines. Antitumor properties of all compounds were determined by 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) assay. Cell viability assay for the tested chalcone compounds was performed and thelog⁡IC50values of the compounds were calculated after 24-hour treatment. Our results indicate that the tested chalcone compounds show antitumor activity against MCF-7 and PC-3 cell lines (p<0.05).

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Mustikasari, Kamilia, and Uripto Trisno Santoso. "The Benefits of Chalcone and Its Derivatives as Antibacterial Agents: A Review." BIO Web of Conferences 20 (2020): 03007. http://dx.doi.org/10.1051/bioconf/20202003007.

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Chalcone is a secondary metabolite compound found in plants. Chalcones contain two aryl rings, namely ring A and B which connected to the α,β unsaturated ketones. Chalcone derivatives are synthesized by various substituent groups in both rings, as well as the types of rings. These variations make chalcone and its derivatives, have interesting bioactivity, one of which is antibacterial. This review is considered the chalcone-derived compounds that have antibacterial bioactivity, including methoxy, hydroxy, prenyl, and halogen groups in ring A or B. Besides, there are two forms of these rings as well such as pyrroly l-furany l-chalcones and indoly l-thiopheny l-chalcone. We hope this review is useful for the development of the synthesis of organic compounds and the discovery of new drug design.

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Espíndola, Cecilia. "Some Ways for the Synthesis of Chalcones - New Ways for the Synthesis of Flavon-3-ols." Mini-Reviews in Organic Chemistry 17, no. 6 (August 24, 2020): 647–73. http://dx.doi.org/10.2174/1570193x16666190919111252.

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The flavonoids by their natural properties and their diverse applications are a group of compounds whose study of origin, characteristics and applications has been dedicated to extensive research. For the organic synthesis of chalcones, due to their interest as precursor molecules of different compounds, several pathways have been developed and reported in numerous works. Analyses on the effect of some of these catalysts on chalcone yield (%), with respect to time and reaction temperature are presented here. Given the importance of flavon-3-ols, as compounds of pharmacological interest mainly, new synthesis routes are proposed, in addition to the existing ones. This paper presents the main pathways for the synthesis of chalcones and analyzes their production. New routes for the synthesis of flavon-3-ols that follow the Claisen-Schmidt condensation and the interconversion of melacacidin are proposed.

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Federič, Jozef, and Štefan Toma. "Michael additions to metallocene analogues of chalcones." Collection of Czechoslovak Chemical Communications 52, no. 1 (1987): 174–81. http://dx.doi.org/10.1135/cccc19870174.

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Eleven analogues of chalcones were synthesized; the variously substituted ferrocenyl, ruthenocenyl or η5-cyclopentadienyltricarbonylmanganese are attached to the β-carbon of the chalcone double bond. Methyl malonate was added to eight selected chalcones. The effect of an aryl group on the chemical shift difference of diastereotopic -COOCH3 groups is discussed. The Vilsmeier-Haack formylation was employed to prepare 1'-chloro and 1'-bromoferrocenecarbaldehydes. The synthesis of 2-chloroferrocenecarbaldehyde from 2-chloroferrocenylmethyldimethylamine is also described.

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Salotra, Riddhi, and Divya Utreja. "A Comprehensive Appraisal of Chalcones and Their Heterocyclic Analogs as Antimicrobial Agents." Current Organic Chemistry 24, no. 23 (December 28, 2020): 2755–81. http://dx.doi.org/10.2174/1385272824999200922090524.

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Owing to the growing demand for compelling antimicrobial agents, chalcones and their heterocyclic derivatives have engrossed prodigious attention of medicinal chemists as an effective clinical template for the synthesis of such agents on account of their structural diversity and molecular flexibility. Chalcones are considered as a fortunate scaffold in the field of both synthetic as well as natural product chemistry. They are reflected as a remarkable section of logically occurring pharmacophores that possess a comprehensive scale of biological activities, such as anti-cancer, anti-malarial, anti-viral and anti-inflammatory, rendering them with a high degree of assortment and noble therapeutic profile. They act as a crucial intermediate for the synthesis of novel heterocyclic skeletons holding biodynamic behavior. This review emphasizes on different aspects of chalcones including their natural sources, recent synthetic methodologies and evaluation of their anti-microbial potential. It is expected as a persuasive compilation on chalcones that may benefit the experts to design potent and less toxic chalcone referents as medicinal agents.

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Journal, Baghdad Science. "Synthesis and Characterization of Some Novel Oxazine, Thiazine and Pyrazol Derivatives." Baghdad Science Journal 13, no. 2 (June 5, 2016): 244–52. http://dx.doi.org/10.21123/bsj.13.2.244-252.

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In this paper, some chalcone derivatives (C1, C2) were synthesized based on the reaction of equal amount of substituted acetophenone and substituted banzaldehyde in basic medium. Oxazine and thiazine derivatives were prepared from the reaction of chalcones (C1-C2) with urea and thiourea respectively in a basic medium. Pyrazole derivatives were prepared based on the reaction of chalcones with hydrazine mono hydrate or phenyl hydrazine in the presence of glacial acetic acid as a catalyst. The new synthesized compounds were identified using various physical techniques like1 H-NMR and FT-IR spectra.

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Pragi, Jagdeep Singh Dua, and Jitender Singh. "Chalcone Ditosylates as Potent Precursor for Synthesis of Some 4,5-Disubstituted Isoxazoles with Antioxidant and Anti-inflammatory Activities." Asian Journal of Chemistry 31, no. 8 (June 28, 2019): 1847–50. http://dx.doi.org/10.14233/ajchem.2019.22077.

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The present work emphasizes on the synthesis of a series of 4,5-disubstituted isoxazole derivatives of α,β-chalcone ditosylates which were synthesized by the reaction of α,β-chalcone ditosylates with hydroxylamine hydrochloride. Various α,β-chalcone ditosylates were prepared by the reaction of respective chalcones with hydroxyl (tosyloxy)iodobenzene.The synthesized compounds were characterized and subsequently evaluated for anti-inflammatory and antioxidant properties.

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Sîrbu, Dumitru, and Ion Marin. "Synthesis and Characterization of [(5-Mercapto-1,3,4-Oxadiazol-2-YL)Aryl]-3,5-Diaryl-4,5-Dihydro-1H-Pyrazole-1-Carbothioamides." Chemistry Journal of Moldova 6, no. 1 (June 2011): 86–89. http://dx.doi.org/10.19261/cjm.2011.06(1).05.

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This article reports on the high yield synthesis and novel chalcones with isothiocyanate and imidazol groups. The synthesis was started from N,N-diphenilamine and finished with 4-(N,N-diphenylamino)-4’-(2-thioxo-imidazolidin-4-one)-chalcone, where the cheap and accessible reagents were used.

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Zhao, Haiying, Xueyou Zhu, Dong Wang, Shufeng Chen, and Zhanxi Bian. "Synthesis, Electrochemical, and Thermal Properties of [3]Ferrocenophane-Containing Chalcone Derivatives." Australian Journal of Chemistry 68, no. 7 (2015): 1035. http://dx.doi.org/10.1071/ch14529.

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[3]Ferrocenophane-containing chalcone derivatives with benzene ring (3a–3d) or naphthalene ring (3e–3f) were synthesized and characterized. The potentials for [3]ferrocenophane-containing chalcones cathodically shifted ~70–80 mV compared with those of ferrocene-containing chalcones, indicating easier oxidation by loss of an electron for the former. The thermal behaviours of the prepared compounds were studied by differential scanning calorimetry and polarizing optical microscopy. Compound 3f with terminal alkyl chain of 14 carbon atoms displayed mesophases, whereas other compounds were non-mesomorphic and showed either crystal polymorphic phase transitions or simple melting and freezing process in the heating and cooling cycles.

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Mitrev, Yavor, Aleksander Mehandzhiyski, Daniela Batovska, Andreas Liese, and Boris Galunsky. "Original enzyme-catalyzed synthesis of chalcones: Utilization of hydrolase promiscuity." Journal of the Serbian Chemical Society 81, no. 11 (2016): 1231–37. http://dx.doi.org/10.2298/jsc160422069m.

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E-chalcone was obtained with very high stereoselectivity for the first time by an enzyme-catalyzed Claisen-Schmidt condensation between benzaldehyde and acetophenone. From a set of lipases, only that from hog pancreas demonstrated promiscuity, catalyzing the reaction in the presence of imidazole as a promoter. Another enzyme, acylase from Aspergillus melleus (3.5.1.14) also proved to be active in the synthesis of E-chalcone under the same reaction conditions. This acylase along with the recombinant D-aminoacylase (3.5.1.81) catalyzed also the reaction between acetophenone and p-nitrobenzaldehyde. Such ?green? approach to synthesis of chalcones is of great interest, because of their important applications as formula ingredients in pharmaceutical, food and cosmetic industry.

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Çelik, Gonca. "New chalcone-3-O-glycoside derivatives: Synthesis and characterization." Journal of Chemical Research 44, no. 9-10 (April 19, 2020): 598–601. http://dx.doi.org/10.1177/1747519820915165.

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Seven novel carbohydrate conjugates of new chalcone-3- O-glycosides were synthesized and characterized. Starting from the substituted 3′-hydroxyarylmethylacetophenone derivatives (chalcones) with α-acetobromoglucose in anhydrous acetone were synthesized 2,3,4,6-tetra- O-acetyl-3′- O-β-d-glucopyranosyloxychalcones. Deblocking the latter with CH3ONa in dry methanol results in substituted chalcone-3- O-glycosides (3′- O-β-d-glucopyranosyloxychalcones). The structures of the newly synthesized chalcone-3- O-glycosides were characterized based on 1H nuclear magnetic resonance, 13C nuclear magnetic resonance, mass spectroscopy, and Fourier-transform infrared spectroscopy.

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Ali, R., A. Rahim, and A. Islam. "Synthesis and Antimicrobial Activity of 7-Hydroxy-3',4'-Methylenedioxy- and 7-Benzyloxy-3',4'-Methylenedioxy Flavanones." Journal of Scientific Research 9, no. 3 (September 1, 2017): 297–306. http://dx.doi.org/10.3329/jsr.v9i3.31229.

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7-Hydroxy-3',4'-methylenedioxy- and 7-benzyloxy-3',4'-methylenedioxy flavanones have been synthesized starting from 2,4-dihydroxyacetophenone. Subsequently biocidal activities of the flavanones have been investigated along with their corresponding chalcones against some bacterial and fungal strains. 2'-Hydroxy-4'-benzyloxy-3,4-methylenedioxy chalcone (5) and its corresponding flavanone (7) showed good antibacterial and antifungal activities against some selected bacterial and fungal strains. On the other hand, 2',4'-dihydroxy-3,4-methylenedioxy chalcone (4) showed no antibacterial and antifungal activities while its corresponding flavanone (6) showed a little antibacterial activity only at higher concentration but did not show antifungal activity. The synthesized chalcones and flavanones have been characterized using UV-Vis, IR and 1H NMRspectral data together with elemental analysis.

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Arslan, Tayfun. "Synthesis and Characterisation of New Sulfonamide Chalcones Containing an azo Group." Journal of Chemical Research 42, no. 5 (May 1, 2018): 267–70. http://dx.doi.org/10.3184/174751918x15269091219930.

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The synthesis and characterisation of a new type of chalcone bearing a –N=N– bond is reported using an environmentally benign approach. The synthesis consists of two steps. ( E)-4-((5-acetyl-2-hydroxyphenyl)diazenyl)benzenesulfonamide was synthesised by an easy structural modification of sulfanilamide. The key step then involved the solvent-free Claisen–Schmidt condensation of benzaldehydes to form the chalcones. The structures of all compounds were confirmed by FTIR, NMR and MS spectroscopy.

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Srikrishna, Devulapally, and Pramod Kumar Dubey. "Synthesis of Novel Hybrid Scaffolds of Pyran Chalcone Derivatives Bearing Indole and Pyrrole Rings." Letters in Organic Chemistry 16, no. 6 (April 23, 2019): 454–61. http://dx.doi.org/10.2174/1570178616666181116110107.

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A series of novel hydroxy-pyran–chalcone hybrid compounds 4(a-b), 5(a-f), 7(a-b) & 8(a-f) has been synthesized by employing simple methods in various approaches through convergent synthetic strategies. 4-hydroxy-3-acetylcoumarin and 3-acetyl-4-hydroxy-6-methyl-2H-pyran-2-one have been used as starting materials and were condensed with indole aldehyde, pyrrole aldehydes independently to give the corresponding chalcones. To further explore, alkylation studies have been carried out on the synthesized hybrid chalcones. The synthesized compounds were established on the basis of IR, HRMS, 1HNMR and 13CNMR spectral data.

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Zhang, Jing, Xin-Ling Fu, Nan Yang, and Qiu-An Wang. "Synthesis and Cytotoxicity of Chalcones and 5-Deoxyflavonoids." Scientific World Journal 2013 (2013): 1–6. http://dx.doi.org/10.1155/2013/649485.

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Chalcones1~8and 5-deoxyflavonoids9~22were synthesized in good yields by aldol condensation, Algar-Flynn-Oyamada reaction, glycosidation, and deacetylation reaction, respectively, starting from 2-acetyl phenols substituted by methoxy or methoxymethoxy group and appropriately benzaldehydes substituted by methoxy, methoxymethoxy group, or chlorine. Among them,13and17~22are new compounds. The cytotoxicity bioassays of these chalcones and 5-deoxyflavonoids were screened using the sulforhodamine B (SRB) protein staining method, and the results showed that compounds2, 4, 5, 6, 10, 15, and19exhibited moderate cytotoxicity against the cancer cell line of MDA-MB-231, U251, BGC-823, and B16 in comparison with control drugs (HCPT, Vincristine, and Taxol).

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Pj, Jainey, and Ishwar Bhat K. "SYNTHESIS, IN SILICO PHYSICOCHEMICAL PROPERTIES AND BIOLOGICAL ACTIVITIES OF SOME PYRAZOLINE DERIVATIVES." Asian Journal of Pharmaceutical and Clinical Research 10, no. 4 (April 1, 2017): 456. http://dx.doi.org/10.22159/ajpcr.2017.v10i4.17093.

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Objectives: Nitrogen containing heterocyclic compounds plays an important role in medicinal chemistry. Among them, five-membered ring pyrazolines have found to possess many biological and pharmacological activities like anticancer, antitubercular, antimicrobial, anti-inflammatory etc. Objective is to determine the physicochemical and drug like properties of the synthesized pyrazolines by in silico methods and to screen their antidiabetic and antioxidant activities.Methods: Chalcones were synthesized from naphthaldehydes by condensing with various substituted acetophenones in ethanol and cyclized into pyrazolines using semicarbazides/thiosemicarbazides by conventional and microwave oven synthesis. The physicochemical and drug like properties were determined by using computational tools. Antidiabetic activity was evaluated by alpha amylase inhibition assay method. Antioxidant activity studies were done by DPPH and nitric oxide method.Results: Pyrazolines were synthesized from chalcones. Microwave irradiated synthesis of chalcone was carried out to get higher yield with less reaction time period as compared to conventional method. The synthesized pyrazolines produces yield around 68% (conventional) and 85% (microwave). In silico studies showed considerable values satisfying all the parameters of physicochemical and Lipinski’s rule of five properties. Among the compounds tested for antidiabetic and antioxidant studies, some showed promising activity.Conclusion: Physiochemical and drug like properties revealed that these compounds have good bioavailability and druglikeness properties. So these compounds are found to be interesting lead molecules for further synthesis as antidiabetic and antioxidant agents.Keywords: Chalcones, pyrazolines, in silico physicochemical properties, biological activities.

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Arasavelli, Ananda Mohan, Ganapavarapu Veera Raghava Sharma, and Siddaiah Vidavalur. "Design, synthesis, and anticancer activity of novel aryl/heteroaryl chalcone derivatives." Heterocyclic Communications 22, no. 1 (February 1, 2016): 1–5. http://dx.doi.org/10.1515/hc-2015-0271.

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AbstractA new series of chalcones 5a–l were synthesized and evaluated for in vitro antiproliferative activity against human colon cancer cell lines. The synthesis of the key intermediate compounds 3a–d was achieved by tetrakis(triphenylphosphine) palladium(II) mediated Suzuki cross coupling reaction. Chalcone 5a shows superior anticancer activity with IC50 value of 21.0 μg/mL compared to the IC50 value of the reference drug doxorubicin at 21.65 μg/mL.

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Ismailova, Gulzira, Shakhnoza Abzalova, Zulfiya Ikramova, Bakhromkhodja Aykhodjaev, and Sabirdjan Arifdjanov. "Synthesis of Some Substituted Analogues of Natural Flavones and Chalcones." International Journal of Psychosocial Rehabilitation 24, Special Issue 1 (February 28, 2020): 840–44. http://dx.doi.org/10.37200/ijpr/v24sp1/pr201226.

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Begum, Shaheen, Arifa Begum, and Bharathi Koganti. "Synthesis and Evaluation of Central Antinociceptive activity of Ring Substituted Chalcones; Molecular Docking Studies with Monoacylglycerol Lipase (MAGL) Enzyme." Oriental Journal of Chemistry 34, no. 4 (July 24, 2018): 1890–97. http://dx.doi.org/10.13005/ojc/3404024.

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Chalcones possess Michael acceptor property due to the presence of α,β-unsaturated enone moiety in their structure. In the present study, molecular docking was performed to predict binding affinity of ring substituted chalcones with Monoacylglycerol lipase (MAGL), a serine hydrolase enzyme which can inhibited by Michael acceptors such as maleimide derivatives. 3, 4-Dimethoxy derivative, 3h, with -44.45 kJmol-1 of interaction energy, exhibited highest binding affinity and formed Pi-Sulphur interactions with methionine-123 residue of MAGL enzyme. As MAGL is an emerging target for antinociceptive drug development, ring substituted chalcones were synthesized and evaluated for their central antinociceptive activity using tail immersion and hot plate methods. The results revealed that compound 3h, chalcone bearing methoxy groups at 3rd and 4th positions of phenyl ring exhibited good antinociceptive activity in both the models. Good correlation was observed between antinociceptive activity and binding affinity toward MAGL in case of compound 3h.

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Lutsky, Eugene, Svyatoslav Fedorovich, Vadim Vyalkov, and Maria Sundyreva. "The influence of downy mildew tolerance of grape varieties on the biosynthesis of stilbenes in callus as potential sources of bioactive substances." BIO Web of Conferences 25 (2020): 02013. http://dx.doi.org/10.1051/bioconf/20202502013.

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Stilbenes represent a considerable practical interest in relation to their benifits to the human health. Callus culture of the grape, which is a natural producer of stilbenes, can serve as an effective source of these compounds. Grape’s resistance to biotic environmental stress conditions is associated with the synthesis and conversion of stilbenes, therefore the aim of the current study was to determine an interrelation between the tolerance of grape varieties to downy mildew and stilbene biosynthesis in the callus culture. Obtained results showed that there was no link between variety’s tolerance to downy mildew and content of stilbenes, chalcones and phenoloxydising enzymes in callus. Presence of the stress impact is a necessary condition for the initiation of the variety-specific synthesis of stilbenes. Callus of varieties, in which stilbenes content was higher, was characterized by a lowered expression of the chalcone synthase and chalcone isomerase relative to expression of genes of the stilbene synthase and phenylalanine ammonia liase, which confirms an interrelation between reduced competition for the substrate between two biosynthesis branches of chalcones and stilbenes with production of the latter.

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Murtaza, Shahzad, Khoula Zubair Mir, Adina Tatheer, and Raja Summe Ullah. "Synthesis and Evaluation of Chalcone and its Derivatives as Potential Anticholinergic Agents." Letters in Drug Design & Discovery 16, no. 3 (January 15, 2019): 322–32. http://dx.doi.org/10.2174/1570180815666180523085436.

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Background: Structural similarity in Chalcone and Pyrazoline brought our intention for the analysis of such compounds. This study involved the synthesis of chalcones and their pyrazoline derivatives and their screening as cholinesterase inhibitors. The newly synthesized compounds were also investigated for their antioxidant potential. Methods: Chalcones were synthesized by well-established methods of synthesis and their structural elucidation was carried out by H-NMR, 13C-NMR, Mass spectrometry and FTIR. For the determination of inhibition potency of synthesized compounds, spectrophotometric method was applied whereas, DPPH free radical scavenging method was used to check the antioxidant ability. Results: Chalcones and their pyrazoline derivatives were synthesized and characterised by 1HNMR, 13C-NMR, Mass spectrometry and FTIR. The compounds were screened for their anti- Alzheimer activity, which exhibited that compounds 1g, 1c and 1h, 1g showed strong inhibitory potency against acetylcholinesterase and butyrylcholinesterase, respectively. DPPH radical scavenging method was applied to check anti-oxidant potential of synthesized compounds and results explored that among all the synthesized compounds only compounds 1c and 1b showed strong scavenging potential. Conclusion: Chalcone and their pyrazoline derivatives were synthesized and screened for their anti-Alzheimer and antioxidant potential. The experimental results of anti-Alzheimer activity were compared with molecular docking studies, which showed that compounds 1g, 1c and 1h, 1g were active against AChE and BChE, respectively. Among the synthesized compounds 1c and 1b were found to be most potent antioxidants. These results suggest that compound 1b, 1c, 1g and 1h may further be explored for further developments.

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Safaei-Ghomi, Javad, and Ali Ghasemzadeh. "Ultrasound-assisted synthesis of dihydropyrimidine-2-thiones." Journal of the Serbian Chemical Society 76, no. 5 (2011): 679–84. http://dx.doi.org/10.2298/jsc100212057s.

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Chalcone derivatives were prepared by the condensation of various substituted aryl aldehydes and acetophenone in alkaline ethanol, while pyrimidine-2-thione derivatives were prepared by the combination of chalcones and thiourea under conventional and ultrasonic conditions. Advantages of the ultrasound effect were observed and high yields of the products were obtained after 20-30 min sonication. Characterization and structural elucidation of the products was realized based on chemical, analytical and spectral analyses. The results clearly demonstrated a high efficiency of the ultrasonic systems was achieved in the chemical processes.

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Sathiyamoorthi, K., V. Mala, R. Suresh, S. P. Sakthinathan, D. Kamalakkannan, K. Ranganathan, R. Arulkumaran, et al. "Synthesis, Spectral Correlations and Antimicrobial Activities of some 2-Hydroxyphenyl-Styrylketone." International Letters of Chemistry, Physics and Astronomy 12 (September 2013): 102–19. http://dx.doi.org/10.18052/www.scipress.com/ilcpa.12.102.

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Some 2’-hydroxyphenylchalcones have been synthesized under microwave irradiation by Claisen-Schmidt condensation between substituted 2-hydroxyacetophenone and substituted benzaldehydes using catalytic amount of SiO2-H3PO4. These chalcones were established by their physical constants and spectroscopic data published earlier. The UV, IR, 1H NMR and 13C NMR spectral data of these chalcone have correlated with Hammett substituent constants, F and R parameters. All the compounds have been subjected to screened for antimicrobial activity.

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Sahu, Adarsh, Shweta Mishra, Asmita Gajbhiye, and Ram Kishore Agrawal. "Magnesium Perchlorate Catalyzed Phospha-Michael Addition of Dialkyl Phosphite to Chalcone." Current Organic Synthesis 15, no. 7 (October 16, 2018): 1020–23. http://dx.doi.org/10.2174/2210315508666180103162452.

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Aim and Objective: Phosphonate possesses a broad range of applications ranging from agrochemistry to medicines. Because of the synthetic and biological importance of phosphonate, their chemistry has stimulated an increasing interest. Hence we developed an efficient and eco-friendly Mg(ClO4)2 catalyzed one pot, solvent free synthesis of phosphonate derivatives of chalcones. Materials and Methods: Magnesium perchlorate phosphonate derivatives of chalcones were synthesized. The reactions were executed at room temperature in the presence of Anhydrous Magnesium perchlorate Anhy. Mg(ClO4)2 under solvent free condition, affording high yield of the product. The cardinal significance of the method lies in its uncomplicated and eco- friendly experimental conditions. Results: The PMA method for P-C bond formation, using dialkyl phosphite with chalcone, was performed in the presence of Anhydrous Magnesium perchlorate under solvent free condition. Despite the solvent free condition, the methodology is efficient since it is required only in catalytic amount of Anhy. Mg(ClO4)2 in one pot reaction. Results demonstrated that the catalytic PMA of dimethyl phosphite, diethyl phosphite, diisopropyl phosphite and dibutyl phosphite with chalcone generates desired products with a percentage yield of 60-80%. Conclusion: We have developed a new efficient PMA method for P-C bond formation, using dialkyl phosphite with α,β-unsaturated ketone i.e. chalcone. To the best of our knowledge, Anhy. Mg(ClO4)2 catalyzed phosphamicheal addition of dialkyl phosphite with chalcones was found to be a new and efficient method for various biological applications.

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Tran, Dao, Son Tran, Vi Nguyen, Tri Le, and Minh Thai. "Synthesis, in vitro Acetylcholinesterase Inhibitory Activity Evaluation and Docking Investigation of Some Aromatic Chalcones." MedPharmRes 1, no. 1 (December 10, 2017): 15–25. http://dx.doi.org/10.32895/ump.mpr.1.1.15/suffix.

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In this study, a total of twenty chalcones were synthesized via Claisen-Schmidt condensation reaction and evaluated for their in vitro acetylcholinesterase inhibitory activities using Ellman’s method. Molecular docking studies on acetylcholinesterase were performed to elucidate the interactions between these chalcone derivatives and acetylcholinesterase active site at the molecular level. From the series, six compounds (S1-5 and S17) exhibited strong acetylcholinesterase inhibitory activities with IC50 values below 100 µM compared to the parent unsubstituted chalcone. Compound S17 (4’-amino-2-chlorochalcone) showed the strongest acetylcholinesterase inhibitory activity in the investigated group with IC50 value of 36.10 µM. Molecular modeling studies were consistent with the results of in vitro acetylcholinesterase inhibitory activities, and chalcone S17 could be considered as a potential lead compound for the development of new acetylcholinesterase inhibitors.

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Rahim, M. A., M. M. H. Bhuiayan, and M. M. Matin. "Microwave Assisted Efficient Synthesis of Some Flavones for Antimicrobial and ADMET Studies." Journal of Scientific Research 12, no. 4 (September 1, 2020): 673–85. http://dx.doi.org/10.3329/jsr.v12i4.45523.

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Microwave (MW) assisted synthetic technique was applied for the preparation of chalcone derivatives 5-7 employing Claisen-Schmidt condensation between 2-hydroxyacetophenone and aromatic aldehydes. These chalcones were further subjected to oxidative cyclization via MW irradiation and furnished the related flavones 8-10 which were characterized by FT-IR, 1H and 13CNMR spectra. The use of these MW assisted reactions provided higher productivity (92-98%) in shorter reaction time (2-6 min) with eco-friendly mild reaction conditions and hence found to be a convenient method as compared to conventional synthesis. These chalcones 5-7, and flavones 8-10 were screened for in vitro antimicrobial activities against five bacterial and three fungal pathogens. The study indicated that they were more active against fungal pathogens than that of bacterial organisms and comparable to the standard antifungal antibiotic nystatin. Interestingly, the prediction of activity spectra for substances (PASS) was also found in agreement with the in vitro results. Some of the compounds were found to have good ADMET properties.

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Ibrayev, M. K., S. B. Akhmetova, A. T. Takibayeva, M. B. Issabayeva, A. O. Nurkenov, and О. T. Seilkhanov. "Synthesis, structure and antimicrobial activity of substituted chalcones and their derivatives." Bulletin of the Karaganda University. "Chemistry" series 95, no. 3 (September 30, 2019): 28–36. http://dx.doi.org/10.31489/2019ch3/28-36.

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37

Pereira, Daniela, Catarina Gonçalves, Beatriz T. Martins, Andreia Palmeira, Vitor Vasconcelos, Madalena Pinto, Joana R. Almeida, Marta Correia-da-Silva, and Honorina Cidade. "Flavonoid Glycosides with a Triazole Moiety for Marine Antifouling Applications: Synthesis and Biological Activity Evaluation." Marine Drugs 19, no. 1 (December 24, 2020): 5. http://dx.doi.org/10.3390/md19010005.

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Over the last decades, antifouling coatings containing biocidal compounds as active ingredients were used to prevent biofouling, and eco-friendly alternatives are needed. Previous research from our group showed that polymethoxylated chalcones and glycosylated flavones obtained by synthesis displayed antifouling activity with low toxicity. In this work, ten new polymethoxylated flavones and chalcones were synthesized for the first time, including eight with a triazole moiety. Eight known flavones and chalcones were also synthesized and tested in order to construct a quantitative structure-activity relationship (QSAR) model for these compounds. Three different antifouling profiles were found: three compounds (1b, 11a and 11b) exhibited anti-settlement activity against a macrofouling species (Mytilus galloprovincialis), two compounds (6a and 6b) exhibited inhibitory activity against the biofilm-forming marine bacteria Roseobacter litoralis and one compound (7b) exhibited activity against both mussel larvae and microalgae Navicula sp. Hydrogen bonding acceptor ability of the molecule was the most significant descriptor contributing positively to the mussel larvae anti-settlement activity and, in fact, the triazolyl glycosylated chalcone 7b was the most potent compound against this species. The most promising compounds were not toxic to Artemia salina, highlighting the importance of pursuing the development of new synthetic antifouling agents as an ecofriendly and sustainable alternative for the marine industry.

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Soltani, Siavash Salek, S. Morteza F. Farnia, and Alireza Foroumadi. "Synthesis and Antibacterial Activity of New Chalcones Bearing an Imidazo[ 1,2-a]pyridine Moiety." Current Chemical Biology 15, no. 2 (August 9, 2021): 163–70. http://dx.doi.org/10.2174/2212796815666210223110208.

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Aim and Objective: Herein, A series of new imidazo[1,2-a]pyridine-chalcone derivatives 3a-m were designed and synthesized to find a new class of antibacterial agents. These compounds were prepared by the aldol condensation of 2-phenylimidazo[1,2-a]pyridine-3-carbaldehyde 2a-b with acetophenone derivatives and other aromatic acetyls. High reaction yields were obtained in a short reaction time, through applying this multi-step pathway. Materials and Methods: In vitro antibacterial activities of the synthesized imidazo[1,2-a]pyridinechalcones were measured against S. aureus, B. subtilis and E. coli with MIC values of 32 -128 μg/mL. Finally, essential structural analyses such as CHN and NMR spectroscopies were used to identify the synthesized chalcones based on imidazo[1,2-a]pyridine derivatives. Results: The results showed that most of the products presented moderate to good antibacterial activities. Compounds 3b, 3d, 3g, 3l and 3m revealed obvious potency against S. aureus, B. subtilis and E. coli with MIC values of 32 μg/mL and 64 μg/mL, which were better when compared with other chalcones. Conclusion: The synthesized antibacterial compounds were obtained with appealing advantages such as high purity, simple pathway, good to excellent yields, inexpensive and easy availability of materials as well as good activities against bacteria. So in this work, a new class of antibacterial chalcones based on imidazo[1,2-a]pyridine has been reported.

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Tran, Thai-Son, Minh-Tri Le, Thi-Cam-Vi Nguyen, The-Huan Tran, Thanh-Dao Tran, and Khac-Minh Thai. "Synthesis, In Silico and In Vitro Evaluation for Acetylcholinesterase and BACE-1 Inhibitory Activity of Some N-Substituted-4-Phenothiazine-Chalcones." Molecules 25, no. 17 (August 27, 2020): 3916. http://dx.doi.org/10.3390/molecules25173916.

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Acetylcholinesterase (AChE) and beta-secretase (BACE-1) are two attractive targets in the discovery of novel substances that could control multiple aspects of Alzheimer’s disease (AD). Chalcones are the flavonoid derivatives with diverse bioactivities, including AChE and BACE-1 inhibition. In this study, a series of N-substituted-4-phenothiazine-chalcones was synthesized and tested for AChE and BACE-1 inhibitory activities. In silico models, including two-dimensional quantitative structure–activity relationship (2D-QSAR) for AChE and BACE-1 inhibitors, and molecular docking investigation, were developed to elucidate the experimental process. The results indicated that 13 chalcone derivatives were synthesized with relatively high yields (39–81%). The bioactivities of these substances were examined with pIC50 3.73–5.96 (AChE) and 5.20–6.81 (BACE-1). Eleven of synthesized chalcones had completely new structures. Two substances AC4 and AC12 exhibited the highest biological activities on both AChE and BACE-1. These substances could be employed for further researches. In addition to this, the present study results suggested that, by using a combination of two types of predictive models, 2D-QSAR and molecular docking, it was possible to estimate the biological activities of the prepared compounds with relatively high accuracy.

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Do, Ha Tuong, and Dao Thanh Tran. "SYNTHESIS OF SOME FLAVONES AND 4-THIOFLAVONES AS POTENT ANTIBACTERIAL AGENTS." Science and Technology Development Journal 12, no. 3 (February 15, 2009): 33–39. http://dx.doi.org/10.32508/stdj.v12i3.2217.

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A series of flavones and thioflavones were synthesized via the chalcone pathway, in which 2'-hydroxyacetophenone is condensed with benzaldehyde derivatives in the medium of potassium hydroxide - methanol at room temperature. The obtained chalcones were treated by iodine in refluxed dimethyl sulfoxide turning into the corresponding flavones. Reaction of flavones and Lawesson's reagent in boiling toluene gave the 4-thioflavones with high yields from 53-76%. All the synthetic compounds were purified by column chromatography and recorded their UV, IR and 'H-NMR spectra.

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41

Palleros, Daniel R. "Solvent-Free Synthesis of Chalcones." Journal of Chemical Education 81, no. 9 (September 2004): 1345. http://dx.doi.org/10.1021/ed081p1345.

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Braun, Roland U., Markus Ansorge, and Thomas J. J. Müller. "Coupling–Isomerization Synthesis of Chalcones." Chemistry - A European Journal 12, no. 35 (December 4, 2006): 9081–94. http://dx.doi.org/10.1002/chem.200600530.

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Malani, M. H., and B. Z. Dholakiya. "Synthesis of carbazonyloxy-based chalcones." Research on Chemical Intermediates 39, no. 3 (June 29, 2012): 1089–100. http://dx.doi.org/10.1007/s11164-012-0668-9.

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Nielsen, Simon Feldbæk, Ming Chen, Thor G. Theander, Arsalan Kharazmi, and S. Brøgger Christensen. "Synthesis of antiparasitic licorice chalcones." Bioorganic & Medicinal Chemistry Letters 5, no. 5 (March 1995): 449–52. http://dx.doi.org/10.1016/0960-894x(95)00053-v.

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Sridevi, CH, K. Balaji, and A. Naidu. "Synthesis and Pharmacological Evaluation of Some Phenylpyrazolo Indoquinoxaline Derivatives." E-Journal of Chemistry 8, no. 2 (2011): 924–30. http://dx.doi.org/10.1155/2011/584817.

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Indoloquinoxalin was fused with 2,3 diphenyl quinoxaline by a methylene bridge which was then allowed for acetylation. The acetylated product was made to react with different aromatic aldehydes to give chalcones. Chalcones refluxed with substituted acid hydrazides to afford different indoloquinoxaline pyrazolines. The structure of chalcones and indoloquinoxaline pyrazolines were confirmed byM.P,TLCand spectral data. All the synthesized compounds were screened for their antioxidant, anti-inflammatory and antihistamic activities.

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Hilma, Rahmiwati, Jasril, and Hilwan Yuda Teruna. "SINTESIS CALKON ((E)-1,3-DI(NAPHTHALEN-2-YL)PROP-2-EN-1-ONE) DAN AKTIVITASNYA SEBAGAI ANTIOKSIDAN." Photon: Jurnal Sain dan Kesehatan 3, no. 1 (October 30, 2012): 7–14. http://dx.doi.org/10.37859/jp.v3i1.143.

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Study on chalcone calkon (E)-1,3-di(naphthalen-2-yl)prop-2-en-1-one synthesis have been carried out with stirrer methode. These compounds can be used as intermediate compound to synthesize others compounds which was reported having antimicrobial, anti-inflammatory, anti-depressant, anti-tumour. The of chalcones synthesis vatives were reported in acid and alkali condition. In this study, chalcone and its derivates were synthesized by using stirrer method in alkaline condition in room temperature. the compounds subjected to somes analyses including melting point measurement, thin layer chromatography and HPLC. Scavenging free radical by using DPPH methode showed Scavenging free radical with LC50 >80 μg/ml min potent activity while the ascorbat acid LC50 89,79 μg/ml.

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Polat, M. Fatih, and Derya Aktaş Anı. "Synthesis and characterization of novel mono, bis and tris heteroaryl chalcone derivatives of 1,3,5-trimethoxybenzene." Organic Communications 14, no. 1 (March 26, 2021): 39–47. http://dx.doi.org/10.25135/acg.oc.95.21.01.1942.

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In this study, a new series consisting of 12 heteroaryl chalcone derivatives of 1,3,5-trimethoxybenzene were synthesised. Chalcones were synthesised in high purity and efficiency, via condensation of mono, bis and tris 2,4,6-trimethoxy acetophenones with hetero-2-carbaldehyde derivatives based on Claisen Schdmit condensation. The reactions feature a good scope for the all products, mild reaction conditions and good yields. The synthesized compounds were characterized by using FT-IR, NMR and elemental analysis spectroscopic techniques.

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Wagh, Sandip, and Ganesh Dhage. "Primary-Secondary Diamine Catalyzed Enantioselective Synthesis of Substituted Cyclohex-2-enones by Cascade Michael–Aldol–Dehydration of Ketones with Chalcones." Synlett 28, no. 11 (March 20, 2017): 1353–57. http://dx.doi.org/10.1055/s-0036-1588976.

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A simple primary-secondary diamine organocatalyst catalyzes the cascade Michael–aldol–dehydration of chalcones and unmodified ketones to produce substituted cyclohex-2-enones under mild conditions with good yields and high enantio- and/or diastereoselectivities. The success of the catalyst system is possibly due to simultaneous activation of the electrophilic chalcone by iminium formation and the nucleophilic ketone by enamine formation with an overall intramolecular iminium–di-enamine mechanism.

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Doan, Tan Nhut, and Dao Thanh Tran. "Synthesis, Antioxidant and Antimicrobial Activities of a Novel Series of Chalcones, Pyrazolic Chalcones, and Allylic Chalcones." Pharmacology & Pharmacy 02, no. 04 (2011): 282–88. http://dx.doi.org/10.4236/pp.2011.24036.

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Sie, Carolynne Zie Wei, Zainab Ngaini, Nurashikin Suhaili, and Eswaran Madiahlagan. "Synthesis of Kojic Ester Derivatives as Potential Antibacterial Agent." Journal of Chemistry 2018 (2018): 1–7. http://dx.doi.org/10.1155/2018/1245712.

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The search for lead product with beneficial pharmacological properties has become a great challenge and costly. Extraction and synthetic modification of bioactive compounds from natural resources has gained great attention and is cost effective. In this study, kojic acid was produced from fungal fermentation, using sago waste as substrate, and chemically incorporated with chalcones and azobenzene to form a series of kojic ester derivatives and evaluated for antibacterial activities. Kojic ester bearing halogenated chalcone demonstrated active inhibition against Staphylococcus aureus compared to that of standard ampicillin. The inhibition increased as the electronegativity of halogens decreased, while incorporation of azobenzene derivatives on kojic acid backbone demonstrated fair antibacterial activity against Escherichia coli with minimum inhibitory concentration (MIC) of 190–330 ppm. The presence of C=C and N=N reactive moieties in both chalcone and azo molecules contributed to the potential biological activities of the kojic acid ester.

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Journal articles on the topic 'Synthesis of chalcones'

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