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Journal articles on the topic 'Methoxy Chalcones'

Author: Grafiati

Published: 5 June 2025

Last updated: 1 August 2025

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1

Olender, Dorota, Anna Pawełczyk, Anna Leśków, Katarzyna Sowa-Kasprzak, Lucjusz Zaprutko, and Dorota Diakowska. "Synthesis of bis-Chalcones Based on Green Chemistry Strategies and Their Cytotoxicity Toward Human MeWo and A375 Melanoma Cell Lines." Molecules 29, no. 21 (2024): 5171. http://dx.doi.org/10.3390/molecules29215171.

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Chalcone is an aromatic ketone that forms the central core of many important biological compounds. Chalcone derivatives show various biological activities, especially anti-inflammatory, antibacterial, antioxidant, and anticancer activities, and also inhibit melanoma cell growth. In this study, we synthesized chalcone compounds with bis-chalcone’s chemical structure under microwave (MW) and microwave–ultrasound (MW-US) conditions and compared them to chalcones produced using the classical synthesis method. All bis-chalcones were synthesized with terephthalaldehyde and an appropriate aromatic ke

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2

Novilla, Arina, Mustofa Mustofa, Indwiani Astuti, Jumina Jumina, and Hery Suwito. "Cytotoxic Activity of Methoxy-4’amino Chalcone Derivatives Against Leukemia Cell Lines." Molecular and Cellular Biomedical Sciences 3, no. 1 (2019): 34. http://dx.doi.org/10.21705/mcbs.v3i1.44.

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Background: Chemotherapy is a common treatment for leukemia as well as in other cancer treatment. The lack of tumor selectivity and development of multi-drug resistance by chemotherapy caused the development of new strategy in cancer treatment become a pressing need. This study was performed to evaluate the anticancer activity and selectivity of seven derivatives of chalcones against K562 and HL-60 leukemia cell lines. Materials and Methods: The cytotoxicity of chalcone’s seven derivatives (compound 1-7) was tested by using MTS (3-(4,5-dimethylthiazol-2-yl)-5-(3-carboxyme-thoxyphenyl)-2-(4-sul

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3

V.H., Elfi Susanti, and Mulyani S. "GREEN SYNTHESIS, CHARACTERIZATION, AND ANTIBACTERIAL ACTIVITY OF METHOXY CHALCONES." RASAYAN Journal of Chemistry 15, no. 04 (2022): 2459–65. http://dx.doi.org/10.31788/rjc.2022.1546957.

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The purpose of this research is to develop the synthesis of chalcone through a green chemical approach that has the potential as an antibacterial. Chalcone synthesis was carried out using a grinding technique through a Claisen-Schmidt condensation reaction at room temperature for 30 minutes by grinding benzaldehyde (4-bromobenzaldehyde or 4- hydroxybenzaldehyde), 4'-methoxyacetophenone, and NaOH. The reaction product was purified by recrystallization through 96% ethanol. The purity of the compound was tested by TLC. Characterization of chalcones by FT IR, 1HNMR, 13C-NMR, and GC-MS showed that

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4

Darwish, Mahmoud I. M., Ahmed M. Moustafa, Asmaa M. Youssef, et al. "Novel Tetrahydro-[1,2,4]triazolo[3,4-a]isoquinoline Chalcones Suppress Breast Carcinoma through Cell Cycle Arrests and Apoptosis." Molecules 28, no. 8 (2023): 3338. http://dx.doi.org/10.3390/molecules28083338.

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Chalcones are interesting anticancer drug candidates which have attracted much interest due to their unique structure and their extensive biological activity. Various functional modifications in chalcones have been reported, along with their pharmacological properties. In the current study, novel chalcone derivatives with the chemical base of tetrahydro-[1,2,4]triazolo[3,4-a]isoquinolin-3-yl)-3-arylprop-2-en-1-one were synthesized, and the structure of their molecules was confirmed through NMR spectroscopy. The antitumor activity of these newly synthesized chalcone derivatives was tested on mo

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5

Popova, Milena, Vassya Bankova, Stefan Spassov, et al. "New Bioactive Chalcones in Propolis from El Salvador." Zeitschrift für Naturforschung C 56, no. 7-8 (2001): 593–96. http://dx.doi.org/10.1515/znc-2001-7-819.

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2′,3′-Dihydroxy-4,4′-dimethoxychalcone (1) and 2′,3′,4-trihydroxy-4′-methoxy-chalcone, two new chalcones, were isolated from propolis from El Salvador. The compounds showed significant antibacterial ana antifunfag activity and moderate toxicity to Artemia salina nauplii

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6

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 obt

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7

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

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8

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

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9

Mulyana, Fathoni Ega, Stephanus Satria Wira Waskitha, Deni Pranowo, Melati Khairuddean, and Tutik Dwi Wahyumingsih. "Synthesis of chalcone derivatives with methoxybenzene and pyridine moieties as potential antimalarial agents." Pharmacia 70, no. 4 (2023): 1305–13. http://dx.doi.org/10.3897/pharmacia.70.e107406.

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Malaria remains an endemic disease in tropical regions, urgently needed the search for effective antimalarial agents due to resistance against existing drugs. This study investigated the potential antimalarial activity of pyridine-based chalcone derivatives against P. falciparum 3D7 and FCR3 strains. The chalcones were synthesized through a one-pot method using various pyridine carbaldehyde, resulting in yields ranging from 53.74 to 86.37%, and all products were characterized using FTIR, GC-MS, and NMR spectroscopies. Among the six chalcones tested, chalcone A [1-(2-methoxyphenyl)-3-(pyridin-2

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10

Mulyana, Fathoni Ega, Stephanus Satria Wira Waskitha, Deni Pranowo, Melati Khairuddean, and Tutik Dwi Wahyumingsih. "Synthesis of chalcone derivatives with methoxybenzene and pyridine moieties as potential antimalarial agents." Pharmacia 70, no. (4) (2023): 1305–13. https://doi.org/10.3897/pharmacia.70.e107406.

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Malaria remains an endemic disease in tropical regions, urgently needed the search for effective antimalarial agents due to resistance against existing drugs. This study investigated the potential antimalarial activity of pyridine-based chalcone derivatives against <i>P. falciparum</i> 3D7 and FCR3 strains. The chalcones were synthesized through a one-pot method using various pyridine carbaldehyde, resulting in yields ranging from 53.74 to 86.37%, and all products were characterized using FTIR, GC-MS, and NMR spectroscopies. Among the six chalcones tested, chalcone A [1-(2-methoxyphenyl)-3-(py

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11

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 (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

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12

Łużny, Mateusz, Ewa Kozłowska, Edyta Kostrzewa-Susłow, and Tomasz Janeczko. "Highly Effective, Regiospecific Hydrogenation of Methoxychalcone by Yarrowia lipolytica Enables Production of Food Sweeteners." Catalysts 10, no. 10 (2020): 1135. http://dx.doi.org/10.3390/catal10101135.

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We describe the impact of the number and location of methoxy groups in the structure of chalcones on the speed and efficiency of their transformation by unconventional yeast strains. The effect of substrate concentration on the conversion efficiency in the culture of the Yarrowia lipolytica KCh 71 strain was tested. In the culture of this strain, monomethoxychalcones (2′-hydroxy-2″-, 3″- and 4″-methoxychalcone) were effectively hydrogenated at over 40% to the specific dihydrochalcones at a concentration of 0.5 g/L of medium after just 1 h of incubation. A conversion rate of over 40% was also o

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13

Kostopoulou, Ioanna, Andromachi Tzani, Nestor-Ioannis Polyzos, et al. "Exploring the 2′-Hydroxy-Chalcone Framework for the Development of Dual Antioxidant and Soybean Lipoxygenase Inhibitory Agents." Molecules 26, no. 9 (2021): 2777. http://dx.doi.org/10.3390/molecules26092777.

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2′-hydroxy-chalcones are naturally occurring compounds with a wide array of bioactivity. In an effort to delineate the structural features that favor antioxidant and lipoxygenase (LOX) inhibitory activity, the design, synthesis, and bioactivity profile of a series of 2′-hydroxy-chalcones bearing diverse substituents on rings A and B, are presented. Among all the synthesized derivatives, chalcone 4b, bearing two hydroxyl substituents on ring B, was found to possess the best combined activity (82.4% DPPH radical scavenging ability, 82.3% inhibition of lipid peroxidation, and satisfactory LOX inh

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14

Monteiro, Patrícia Queiroz, Edgar Schaeffer, Alcides José Monteiro da Silva, Carlos Roberto Alves, and Franklin Souza-Silva. "A Virtual Screening Approach to Evaluate the Multitarget Potential of a Chalcone Library with Binding Properties to Oligopeptidase B and Cysteine Proteinase B from Leishmania (Viannia) braziliensis." International Journal of Molecular Sciences 26, no. 5 (2025): 2025. https://doi.org/10.3390/ijms26052025.

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Leishmaniasis remains a significant public health problem in Brazil, particularly due to Leishmania (Viannia) braziliensis, which is associated with severe dermatological syndromes. The current treatments are limited by toxicity and uncertain efficacy, highlighting the need for new compounds with pharmacological potential. This study investigates chalcones as multitarget binding agents for oligopeptidase B (OPB) and cysteine proteinase B (CPB), which are critical pathogenic determinants of L. (V.) braziliensis. The methodology involved replacing methoxy groups with aryl motifs at various posit

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15

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 (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

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16

M., L. NARWADE, M. CHINCHOLKAR M., and W. SATHF S. "Stability Constants of lron(lll) Chelates with Some Substituted Chalcones at 0.1 M Ionic Strength and at Various Ionic Strengths of 2'-4-ydroxy-4-methoxy5'-methylchalcone." Journal of Indian Chemical Society Vol. 62, Mar 1985 (1985): 194–97. https://doi.org/10.5281/zenodo.6321884.

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Department of Chemistry, Vidarbha Mahavidyalaya, Amravati-444 604 <em>Manuscript received 21<strong><em> </em></strong>September 1981, revised </em>5 <em>September 1983, accepted 19 January<strong> </strong>1985</em> The interaction of Fe<sup>III</sup> with 2'-hydroxy-4-methoxy-5'-methylchalcone (1), 2'- hydroxy-4-methoxychalcone (2), 2'-hydroxy-3'-bromo-4-methoxy-5'-methylchalcone (3) and 2'-hydroxy-4-methoxy-5',6 -benzochalcone (4) has been investigated potentiometrically in 70% dioxane-water mixture at 0.1 M ionic strength. The study of Fe<sup>III</

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17

Kudličková, Zuzana, Radka Michalková, Aneta Salayová, et al. "Design, Synthesis, and Evaluation of Novel Indole Hybrid Chalcones and Their Antiproliferative and Antioxidant Activity." Molecules 28, no. 18 (2023): 6583. http://dx.doi.org/10.3390/molecules28186583.

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The synthesis, anticancer, and antioxidant activities of a series of indole-derived hybrid chalcones are reported here. First, using the well-known Claisen–Schmidt condensation method, a set of 29 chalcones has been designed, synthesized, and consequently characterized. Subsequently, screening for the antiproliferative activity of the synthesized hybrid chalcones was performed on five cancer cell lines (HCT116, HeLa, Jurkat, MDA-MB-231, and MCF7) and two non-cancer cell lines (MCF-10A and Bj-5ta). Chalcone 18c, bearing 1-methoxyindole and catechol structural features, exhibited selective activ

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18

Baisarov, G. M., and S. M. Adekenov. "NEW PHARMACOLOGICALLY ACTIVE COMPOUNDS BASED ON 5-HYDROXY-7-METHOXY-2-PHENYLCHROMAN-4-ONE." Chemical Journal of Kazakhstan 3 (September 30, 2021): 119–27. http://dx.doi.org/10.51580/2021-1/2710-1185.44.

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The reaction of 5-hydroxy-7-methoxy-2-phenylchroman-4-one with dibromoalkanes in acetone in the presence of potassium carbonate proceeds according to the Michael’s retro-reaction O-alkylation and leads to the formation of the corresponding 2-(bromo-alkoxy) chalcones. The structure of the synthesized compounds was confirmed by IR-, 1H- and 13C-NMR spectroscopy. The cytotoxic, hepatoprotective and anti-inflammatory effects of chalcone derivatives (2-3) were studied for the first time in vitro and in vivo.

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19

S, Sonu, Girendra Kumar Gautam, Arun Kumar Mishra, Baby Rabiya Parveen, and Harpreet singh. "Molecular Docking Studies, Synthesis of Novel Isoxazole Derivatives from 3-Methoxy Substituted Chalcone and Evaluation of their Anti-Inflammatory Activity." Oriental Journal Of Chemistry 39, no. 3 (2023): 675–83. http://dx.doi.org/10.13005/ojc/390318.

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Synthesis of 3-methoxy acetophenone with substituted benzaldehydes resulted in a number of novel chalcones. The chalcones were then treated to a cyclization reaction with hydroxylamine hydrochloride in ethanol to enable the synthesis of 3-methoxy acetophenone isoxazole derivatives. After purification, the structures of the synthesized compounds were identified using TLC, FTIR, 1H NMR, 13C NMR and a Mass spectroscopy. The carrageenan-induced paw edema method was used to test the compounds for anti-inflammatory activity. Based on the findings, the three compounds appeared to be moderate to extre

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20

Napolitano, Hamilton B., Jean M. F. Custodio, Wesley F. Vaz, and Eduardo M. Faria. "Supramolecular arrangement of two methoxy-chalcones." Acta Crystallographica Section A Foundations and Advances 73, a1 (2017): a176. http://dx.doi.org/10.1107/s0108767317098257.

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21

Bolte, M., G. Schütz та H. J. Bader. "Two Nitro-α-methoxy-trans-chalcones". Acta Crystallographica Section C Crystal Structure Communications 52, № 11 (1996): 2807–9. http://dx.doi.org/10.1107/s0108270196007913.

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22

Amor, Evangeline C., Irene M. Villaseñor, M. Nabeel Ghayur, Anwar H. Gilani, and M. Iqbal Choudhary. "Spasmolytic Flavonoids from Syzygium samarangense (Blume) Merr. & L.M. Perry." Zeitschrift für Naturforschung C 60, no. 1-2 (2005): 67–71. http://dx.doi.org/10.1515/znc-2005-1-213.

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The hexane extract of Syzygium samarangense (Ss.Hex) dose-dependently (10D1000 μg/ ml) relaxed the spontaneously contracting isolated rabbit jejunum. Four rare C-methylated flavonoids with a chalcone and a flavanone skeleton were isolated from Ss.Hex and were subsequently tested for spasmolytic activity. All flavonoids, identified as 2′-hydroxy-4′,6′- dimethoxy-3′-methylchalcone (1), 2′,4′-dihydroxy-6′-methoxy-3′,5′-dimethylchalcone (2), 2′,4′-dihydroxy-6′-methoxy-3′-methylchalcone (3), and 7-hydroxy-5-methoxy-6,8-dimethylflavanone (4), showed dose-dependent spasmolytic activity in the rabbit

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23

Salim, Inas, Ahmed M. Abdula, and Abdulkadir Mohammed Noori Jassim. "Synthesis, characterization of 3,5-disubstitutedaryl-4,5-dihydro-1H-pyrazole-1-carbothioamide derivatives and evaluation of their antioxidant activity." Journal of Kufa for Chemical Sciences 4, no. 1 (2024): 175–91. https://doi.org/10.36329/jkcm/2024/v4.i1.13975.

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The pyrazolines are nitrogen-containing heterocyclic structures with five members that are used in the production of pharmaceuticals and organic materials. The goal of this work was to preparation and characterization a novel series of derivatives of 3,5-disubstitutedaryl-4,5-dihydro-1H-pyrazole-1-carbothioamide. Two steps were taken in the synthesis of the novel derivatives from chalcones: the first step chalcones was prepared from reaction of {3,4-(methylenedioxy) acetophenone or para methoxy acetophenone} with various aldehydes (previously prepared) in Claisen-Schmidt condensation at room t

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24

Peerzade, Nargisbano A., Shravan Y. Jadhav, and Raghunath B. Bhosale. "Synthesis and Biological Evaluation of Some Novel Quinoline based Chalcones as Potent Antimalarial, Anti-inflammatory, Antioxidant and Antidiabetic Agents." Asian Journal of Chemistry 32, no. 4 (2020): 959–64. http://dx.doi.org/10.14233/ajchem.2020.22542.

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The objective of the present study was to synthesize a series of some novel quinoline based methoxy substituted chalcones and to evaluate their in vitro antimalarial, anti-inflammatory, antioxidant and antidiabetic activitites. The quinoline based chalcones was synthesized by condensation of 2-chloro-3-formyl qunoline with various methoxy substituted acetophenone in presence of NaOH. The Claisen-Schmidt condensation gave high yield of quinoline based chalcones. Synthesis of 2-chloro-3-formyl quinoline was carried out by Vilsmeir-Haack reaction on acetanilide and 4-methoxy acetanilide which on

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25

Constantinescu, Teodora, and Alin Grig Mihis. "Two Important Anticancer Mechanisms of Natural and Synthetic Chalcones." International Journal of Molecular Sciences 23, no. 19 (2022): 11595. http://dx.doi.org/10.3390/ijms231911595.

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ATP-binding cassette subfamily G and tubulin pharmacological mechanisms decrease the effectiveness of anticancer drugs by modulating drug absorption and by creating tubulin assembly through polymerization. A series of natural and synthetic chalcones have been reported to have very good anticancer activity, with a half-maximal inhibitory concentration lower than 1 µM. By modulation, it is observed in case of the first mechanism that methoxy substituents on the aromatic cycle of acetophenone residue and substitution of phenyl nucleus by a heterocycle and by methoxy or hydroxyl groups have a posi

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26

D., R. GUPTA, KAMALUDDIN, and NAITHANI SHOBHA. "Epoxidation of Chalcones with t-Butylhydroperoxide in Presence of a Cobalt(II) Schiff Base Complex." Journal of Indian Chemical Society Vol. 66, Mar 1989 (1989): 160–63. https://doi.org/10.5281/zenodo.5939979.

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Department of Chemistry, University of Roorkee, Roorkee-217 667 <em>Manuscript received 8 June 1988, revised 15 November 1988, accepted 14 December 1988</em> The epoxidation of some chalcones, i.e. 3-nitrochalcone, 4'-methoxy-3- nitrochalcone, 4'-hydroxy-4-methoxychalcone, 3'-aminochalcone, 3'-amino3-nitrochalcone, 2-methoxychalcone and 2-hydroxy-chalcone has been carried out with t-butylhydroperoxide using cobalt(II) Schiff' base complex as a catalyst. The effects of solvent, temperature, different substituents and quantity of catalyst on the yield of the epoxides have als

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27

Dhivare, Ravindra S., and S. S. Rajput. "Microwave Supported Synthesis and Antimicrobial Evaluation of Bis-Pyrazole Derivatives from N-Phenyl Glutarimides." International Letters of Chemistry, Physics and Astronomy 65 (April 2016): 53–63. http://dx.doi.org/10.18052/www.scipress.com/ilcpa.65.53.

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A simple ecofriendly microwave supported solvent free synthesis of bis-chalcones was carried out by the reaction of di-substituted 4-hydroxy-3-methoxy benzaldehyde with different substituted N-phenylpiperidine-2,6-diones in presence of neutral corundum. By the same way the novel bis-pyrazoles were developed from bis-chalcones and hydrazine hydrate with neutral corundum. All the derivatives were characterized and screened their antimicrobial potencies.

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Dhivare, Ravindra S., and S. S. Rajput. "Microwave Supported Synthesis and Antimicrobial Evaluation of Bis-Pyrazole Derivatives from N-Phenyl Glutarimides." International Letters of Chemistry, Physics and Astronomy 65 (April 6, 2016): 53–63. http://dx.doi.org/10.56431/p-rk8792.

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A simple ecofriendly microwave supported solvent free synthesis of bis-chalcones was carried out by the reaction of di-substituted 4-hydroxy-3-methoxy benzaldehyde with different substituted N-phenylpiperidine-2,6-diones in presence of neutral corundum. By the same way the novel bis-pyrazoles were developed from bis-chalcones and hydrazine hydrate with neutral corundum. All the derivatives were characterized and screened their antimicrobial potencies.

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29

Ravindra, S. Dhivare, and S. Rajput S. "Microwave supported synthesis and antimicrobial evaluation of bispyrazole derivatives from N-phenyl glutarimides." International Letters of Chemistry, Physics and Astronomy 65 (April 6, 2016): 53–63. https://doi.org/10.18052/www.scipress.com/ILCPA.65.53.

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<strong>Abstract: </strong> A simple eco-friendly microwave supported solvent-free synthesis of <strong><em>bis-chalcones</em></strong> was carried out by the reaction of di-substituted 4-hydroxy-3-methoxy benzaldehyde with different substituted N-phenylpiperidine-2, 6-diones in presence of neutral corundum. By the same way, the novel bis-pyrazoles were developed from bis-chalcones and hydrazine hydrate with neutral corundum. All the derivatives were characterized and screened their antimicrobial potencies.

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30

Gaigé, Stéphanie, Anne Abysique, Rym Barbouche, et al. "3,5-Dimethyl-2,4,6-trimethoxychalcone Lessens Obesity and MAFLD in Leptin-Deficient ob/ob Mice." International Journal of Molecular Sciences 25, no. 18 (2024): 9838. http://dx.doi.org/10.3390/ijms25189838.

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Chalcones constitute an important group of natural compounds abundant in fruits and comestible plants. They are a subject of increasing interest because of their biological activities, including anti-diabetic and anti-obesity effects. The simple chalcone structural scaffold can be modified at multiple sites with different chemical moieties. Here, we generated an artificial chalcone, i.e., 3,5-dimethyl-2,4,6-trimethoxychalcone (TriMetChalc), derived from 2′,4′-Dihydroxy-6′-methoxy-3′,5′-dimethylchalcone (DMC). DMC is a major compound of Cleistocalyx operculatus, a plant widely used in Asia for

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31

Go, Mei-Lin, Mei Liu, Prapon Wilairat, Philip J. Rosenthal, Kevin J. Saliba, and Kiaran Kirk. "Antiplasmodial Chalcones Inhibit Sorbitol-Induced Hemolysis of Plasmodium falciparum-Infected Erythrocytes." Antimicrobial Agents and Chemotherapy 48, no. 9 (2004): 3241–45. http://dx.doi.org/10.1128/aac.48.9.3241-3245.2004.

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ABSTRACT A series of alkoxylated and hydroxylated chalcones previously reported to have antiplasmodial activities in vitro were investigated for their effects on the new permeation pathways induced by the malaria parasite in the host erythrocyte membrane. Of 21 compounds with good antiplasmodial activities (50% inhibitory concentrations [IC50s], ≤20 μM), 8 members were found to inhibit sorbitol-induced lysis of parasitized erythrocytes to a significant extent (≤40% of control values) at a concentration (10 μM) that was close to their antiplasmodial IC50s. Qualitative structure-activity analysi

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Svarc, Federico. "Synthesis of dibenzoylmethane-flavonoid hybrids as potential uv filters. Hybrids of chalcones." Archives of Clinical and Experimental Pathology 1, no. 1 (2022): 01–07. http://dx.doi.org/10.31579/2834-8508/002.

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Background: It has been reported that chalcones (a family of flavonoids) have activity as UV rays absorbers. Previously we have reported that the compounds2´-hydroxy-4- methoxychalcone and 2´-hydroxy-4-methoxy dibenzoylmethane have the basic properties of UVA filters (both show their maximum absorption in the range 350-370 nm with good photostability) Objective: in this work, we describea new series of chalcone-dibenzoylmethane hybrid candidates as synthetic UV filtersand flavonoids Method: The compounds resultedfrom multi step synthesisstarting from 4-formylbenzoic acid and 2´- hydroxy acetop

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Mathew, Bijo, Githa Elizabeth Mathew, Gulberk Ucar, et al. "Monoamine oxidase inhibitory activity of methoxy-substituted chalcones." International Journal of Biological Macromolecules 104 (November 2017): 1321–29. http://dx.doi.org/10.1016/j.ijbiomac.2017.05.162.

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Shirmila, D. Angeline, D. Reuben Jonathan, M. Krishna Priya, K. Laavanya, J. Hemalatha, and G. Usha. "SYNTHESIS, In-vitro AND In-silico ANTICANCER ACTIVITY STUDIES OF METHOXY SUBSTITUTED TETRALONE-BASED CHALCONE DERIVATIVES." RASAYAN Journal of Chemistry 15, no. 04 (2022): 2249–57. http://dx.doi.org/10.31788/rjc.2022.1547030.

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Chalcones are organic compounds with numerous biotic activities such as anticancer, antibacterial, and antifungal. Using the Claisen-Schmidt condensation reaction, three methoxy substituted chalcone derivatives were synthesized and crystallized using the slow evaporation method. Cytotoxicity evaluation showed that all three compounds were almost inoffensive to VERO cell lines and exhibited excellent anticancer activity on breast cancer (MCF-7) cell lines. Molecular docking analysis confirmed that all three molecules fit well at the active site of the target protein with PDB ID: 1M17. In silico

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Jadhav, P., M. Borkar, K. Malbari, M. Joshi, and M. Kanyalkar. "DESIGN, SYNTHESIS AND MOLECULAR MECHANISM OF FEW NEURAMINIDASE INHIBITORS IN TREATMENT OF H1N1 BY NMR TECHNIQUES." INDIAN DRUGS 56, no. 02 (2019): 7–15. http://dx.doi.org/10.53879/id.56.02.11584.

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Considering the issue of resistance to anti-influenza drugs, there is a need for discovery of new antiviral drugs. In view of this, flavones and their synthetic precursors i.e. chalcones were designed as inhibitors of influenza virus - H1N1 neuraminidase enzyme using structure-based drug design. Based on the best docking scores, some chalcone and flavone derivatives were synthesized and characterized by IR and proton NMR. Few of them were selected for 31P NMR studies, in order to probe the molecular mechanism of their antiviral action. Reasonably good correlation between docking scores and 31P

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Tuerxuntayi, Adila, Tajiguli Abulikemu, and Chao Niu. "Mechanisms of 4-Dimethylamino-4'-Methoxy Chalcone in Promoting Melanin Synthesis." Natural Product Communications 17, no. 3 (2022): 1934578X2210868. http://dx.doi.org/10.1177/1934578x221086895.

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Background and aims: Vitiligo, a pigmentation-associated disease, affects 1–2% of the global population andis difficult to treat. The pathogenetic mechanism of vitiligo remains unclear. Vernonia anthelmintica (L.) Willd. extract for vitiligo treatment was initially recorded 300 years ago. Itschalcone compounds are believed to play essential roles in this treatment. In a previous study, chalcones were shown to enhance melanin production and tyrosinase activity inmouse B16 cells. Materials and methods: In this study, the effects were investigated of 4-dimethylamino-4'-methoxy chalcone (DMC) on t

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Pawlak, Aleksandra, Marta Henklewska, Beatriz Hernández Suárez, et al. "Chalcone Methoxy Derivatives Exhibit Antiproliferative and Proapoptotic Activity on Canine Lymphoma and Leukemia Cells." Molecules 25, no. 19 (2020): 4362. http://dx.doi.org/10.3390/molecules25194362.

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Chalcones are interesting candidates for anti-cancer drugs due to the ease of their synthesis and their extensive biological activity. The study presents antitumor activity of newly synthesized chalcone analogues with a methoxy group on a panel of canine lymphoma and leukemia cell lines. The antiproliferative effect of the 2′-hydroxychalcone and its methoxylated derivatives was evaluated in MTT assay after 48 h of treatment in different concentrations. The proapoptotic activity was studied by cytometric analysis of cells stained with Annexin V/FITC and propidium iodide and by measure caspases

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Dangar, Vikram R. "Synthesis, Characterization and Antimicrobial activities of some new Pyrazole-1-carbothioamide derivatives." International Journal for Research in Applied Science and Engineering Technology 9, no. 11 (2021): 1720–23. http://dx.doi.org/10.22214/ijraset.2021.39002.

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Abstract: Some new 5-Aryl-3-[4’-(o-chlorobenzyloxy)-3’-methoxy-phenyl]-1-carbothioamide-4, 5-dihydro-1H-pyrazole derivatives were prepared. All the prepared compounds were characterized by their spectral (I.R., N. M. R., Mass) data and screened for their antimicrobial activities. Keywords: Chalcones & Pyrazoline derivatives, Antimicrobial activities.

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Perdana, Fitra, Yum Eryanti, and Adel Zamri. "Synthesis and Toxicity Assessments Some Para-methoxy Chalcones Derivatives." Procedia Chemistry 16 (2015): 129–33. http://dx.doi.org/10.1016/j.proche.2015.12.040.

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Elsayed, Galal A., and Ali Kh Khalil. "Facile Synthesis of Chalcone Glycosides Isolated from Aerial Parts of Brassica rapa l. ‘hidabeni'." Current Organic Synthesis 15, no. 3 (2018): 423–29. http://dx.doi.org/10.2174/1570179414666170824161618.

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Background: The Cruciferous family of vegetables which includes Brassica Turnips showed antioxidant and hepatoprotective effects. The phytochemical investigations of the aerial parts of the traditional Japanese turnip vegetable (B. rapa L. 'hidabeni') revealed the presence of three chalcone glycosides, along with other glycoside components. As many natural products inhibited Ag-stimulated degranulation in cellular system, those chalcone glycosides have biological significance of suppressing antigen-stimulated degranulation in rat basophilic leukemia RBL-2H3 cells. Aim and Objective: Further in

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Thebti, Amal, Ahmed Meddeb, Issam Ben Salem, et al. "Antimicrobial Activities and Mode of Flavonoid Actions." Antibiotics 12, no. 2 (2023): 225. http://dx.doi.org/10.3390/antibiotics12020225.

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The emergence of antibiotics-resistant bacteria has been a serious concern for medical professionals over the last decade. Therefore, developing new and effective antimicrobials with modified or different modes of action is a continuing imperative. In this context, our study focuses on evaluating the antimicrobial activity of different chemically synthesized flavonoids (FLAV) to guide the chemical synthesis of effective antimicrobial molecules. A set of 12 synthesized molecules (4 chalcones, 4 flavones and 4 flavanones), bearing substitutions with chlorine and bromine groups at the C6′ positio

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Barros, Ana I. R. N. A., Fernando M. Nunes, Cristina Barros, Artur M. S. Silva, and M. Rosário M. Domingues. "Structural Characterization of Nitrated 2′-Hydroxychalcones by Electrospray Ionization Tandem Mass Spectrometry." European Journal of Mass Spectrometry 15, no. 5 (2009): 605–16. http://dx.doi.org/10.1255/ejms.1020.

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Isomeric 2′-hydroxychalcones bearing nitro and methoxy groups in different positions of their skeleton were analyzed by tandem mass spectrometry (MS/MS) with electrospray ionization (ESI), in positive mode. Collision-induced dissociation of the protonated molecules, [M + H]+, formed under electrospray conditions were studied and it was found that the product ion spectra of these chalcones presented different fragmentation patterns depending on the position of the substituents on the molecule. The product ion spectra (ESI-MS/MS) of the B ring ortho-nitro substituted 2′-hydroxychalcone and of th

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Ravindra, S. Dhivare, and S. Rajput S. "Microwave Assisted Synthesis and Antimicrobial activities of 3,4-bis-(4-hydroxy-3- methoxybenzylidene)-7-(N-phenyl)-3,3a,3b,4,5,7-hexahydro-2H-pyrrolo[2,3-c,5,4-c] di pyrazole." International Journal of Current Trends in Pharmaceutical Research 3, no. 6 (2015): 1106–9. https://doi.org/10.5281/zenodo.3909815.

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<strong>A B S T R A C T</strong> The novel pyrazole derivatives were synthesized by reacting substituted bis-chalcones with 4-hydroxy-3-methoxy benzaldehyde to get 3,4-bis-(4-hydroxy-3-methoxybenzylidene)-7-(N-phenyl)-3,3a,3b,4,5,7-hexahydro -2H-pyrrolo [2,3-c,5,4-c] dipyrazole using the solvent-free microwave method. All these derivatives were screened for antimicrobial activities.

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Kenari, Fatemeh, Szilárd Molnár, and Pál Perjési. "Reaction of Chalcones with Cellular Thiols. The Effect of the 4-Substitution of Chalcones and Protonation State of the Thiols on the Addition Process. Diastereoselective Thiol Addition." Molecules 26, no. 14 (2021): 4332. http://dx.doi.org/10.3390/molecules26144332.

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Several biological effects of chalcones have been reported to be associated with their thiol reactivity. In vivo, the reactions can result in the formation of small-molecule or protein thiol adducts. Both types of reactions can play a role in the biological effects of this class of compounds. Progress of the reaction of 4-methyl- and 4-methoxychalcone with glutathione and N-acetylcysteine was studied by the HPLC-UV-VIS method. The reactions were conducted under three different pH conditions. HPLC-MS measurements confirmed the structure of the formed adducts. The chalcones reacted with both thi

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Păușescu, Iulia, Izolda Kántor, György Babos та ін. "Halochromic Behavior and Anticancer Effect of New Synthetic Anthocyanidins Complexed with β-Cyclodextrin Derivatives". International Journal of Molecular Sciences 23, № 15 (2022): 8103. http://dx.doi.org/10.3390/ijms23158103.

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Anthocyanidins, the aglycons of anthocyanins, are known, beyond their function in plants, also as compounds with a wide range of biological and pharmacological activities, including cytostatic effect against various cancer cells. The nature and position of the substituents in the flavylium cation is essential for such biological properties, as well as the equilibrium between the multistate of the different chemical species that are generated by the flavylium cation, including quinoidal base, hemiketal, and cis- and trans-chalcones. In this work, eight new flavylium derivatives were synthesized

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Jasinski, Jerry P., Ray J. Butcher, Anil N. Mayekar, H. S. Yathirajan, and B. Narayana. "Structures of Three Chalcones Derived from 6-Methoxy-2-naphthaldehyde." Journal of Chemical Crystallography 39, no. 3 (2008): 157–62. http://dx.doi.org/10.1007/s10870-008-9446-3.

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Mistry, Ketan, and K. R. Desai. "Studies on Synthesis of Some New Chalcone and Pyrimidines and their Antibacterial Activity." E-Journal of Chemistry 2, no. 2 (2005): 152–56. http://dx.doi.org/10.1155/2005/690296.

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Pyrimidine-2-one derivatives, 2-[2-{1ʹ-(p-nitrophenyl)-6ʹ-(substituted-phenyl)-pyrimidine-2ʹ-one-4ʹ-yl}-hydrazinomethyl]-3-(p-methoxy phenyl)-quina-zoline-4(3H)-one [4a-j] have been synthesised by the condensation ofp-nitro phenylurea and various chalcones, 2-(substituted phenylchalconylhydrazinomethyl)-3-(p-methoxyphenyl)-quinazoline-4(3H)-one [3a-j] in the presence of catalytic amount of conc. HCl. And this series of chalcones have been synthesised by the reaction of 2-acetylhydrazinomethyl-3-(substitutedphenyl)-quinazoline-4(3H)-one [2] with different substituted aldehydes in presence of a

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Sánchez Vergara, María Elena, María José Canseco Juárez, Ricardo Ballinas Indili, Genaro Carmona Reyes, José Ramón Álvarez Bada, and Cecilio Álvarez Toledano. "Studies on the Structure, Optical, and Electrical Properties of Doped Manganese (III) Phthalocyanine Chloride Films for Optoelectronic Device Applications." Coatings 12, no. 2 (2022): 246. http://dx.doi.org/10.3390/coatings12020246.

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In the last few years, significant advances have been achieved in the development of organic semiconductors for use in optoelectronic devices. This work reports the doping and deposition of semiconducting organic thin films based on manganese (III) phthalocyanine chloride (MnPcCl). In order to enhance the semiconducting properties of the MnPcCl films, different types of pyridine-based chalcones were used as dopants, and their influence on the optical and electric properties of the films was analyzed. The morphology and structure of the films were studied using IR spectroscopy and scanning elec

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Bustos, Luis, Carlos Echiburú-Chau, Alejandro Castro-Alvarez, et al. "Cytotoxic Effects on Breast Cancer Cell Lines of Chalcones Derived from a Natural Precursor and Their Molecular Docking Analysis." Molecules 27, no. 14 (2022): 4387. http://dx.doi.org/10.3390/molecules27144387.

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This study aimed to determine the in vitro cytotoxicity and understand possible cytotoxic mechanisms via an in silico study of eleven chalcones synthesized from two acetophenones. Five were synthesized from a prenylacetophenone isolated from a plant that grows in the Andean region of the Atacama Desert. The cytotoxic activity of all the synthesized chalcones was tested against breast cancer cell lines using an MTT cell proliferation assay. The results suggest that the prenyl group in the A-ring of the methoxy and hydroxyl substituents of the B-ring appear to be crucial for the cytotoxicity of

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Ethiraj, Kannatt Radhakrishnan, Jesil Mathew Aranjani, and Fazlur-Rahman Nawaz Khan. "Synthesis of Methoxy-substituted Chalcones andin vitroEvaluation of their Anticancer Potential." Chemical Biology & Drug Design 82, no. 6 (2013): 732–42. http://dx.doi.org/10.1111/cbdd.12184.

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