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Journal articles on the topic 'Acridine Derivatives'

Author: Grafiati

Published: 4 June 2021

Last updated: 26 July 2025

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1

Galenko, Ekaterina E., Mikhail S. Novikov, Alexander S. Bunev, and Alexander F. Khlebnikov. "Acridine–Isoxazole and Acridine–Azirine Hybrids: Synthesis, Photochemical Transformations in the UV/Visible Radiation Boundary Region, and Anticancer Activity." Molecules 29, no. 7 (2024): 1538. http://dx.doi.org/10.3390/molecules29071538.

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Easy-to-handle N-hydroxyacridinecarbimidoyl chloride hydrochlorides were synthesized as convenient nitrile oxide precursors in the preparation of 3-(acridin-9/2-yl)isoxazole derivatives via 1,3-dipolar cycloaddition with terminal alkynes, 1,1-dichloroethene, and acrylonitrile. Azirines with an acridin-9/2-yl substituent attached directly or via the 1,2,3-triazole linker to the azirine C2 were also synthesized. The three-membered rings of the acridine–azirine hybrids were found to be resistant to irradiation in the UV/visible boundary region, despite their long-wave absorption at 320–420 nm, in

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2

Khunnawutmanotham, Nisachon, Watthanachai Jumpathong, Chatchakorn Eurtivong, Nitirat Chimnoi, and Supanna Techasakul. "Synthesis, cytotoxicity evaluation, and molecular modeling studies of 2,N10-substituted acridones as DNA-intercalating agents." Journal of Chemical Research 44, no. 7-8 (2020): 410–25. http://dx.doi.org/10.1177/1747519820902674.

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Acridine-based compounds possess anticancer activities by intercalating to DNA. Although they have chemotherapeutic potential, acridine-based compounds are not used to treat cancer. In this study, 2, N10-acridone derivatives are designed and synthesized based on acridone, a ketone derivative of acridine. Herein, acridone is functionalized with alkyl side chains containing terminal nitrogen-based moieties at the N10-position and substituted at the C2-position. The products are evaluated for in vitro cytotoxicity against four cancer cell lines: Molt-3, HepG2, A549, and HuCCA-1. The derivative be

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3

Varakumar, Potlapati, Kalirajan Rajagopal, Baliwada Aparna, et al. "Acridine as an Anti-Tumour Agent: A Critical Review." Molecules 28, no. 1 (2022): 193. http://dx.doi.org/10.3390/molecules28010193.

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This review summarized the current breakthroughs in the chemistry of acridines as anti-cancer agents, including new structural and biologically active acridine attributes. Acridine derivatives are a class of compounds that are being extensively researched as potential anti-cancer drugs. Acridines are well-known for their high cytotoxic activity; however, their clinical application is restricted or even excluded as a result of side effects. The photocytotoxicity of propyl acridine acts against leukaemia cell lines, with C1748 being a promising anti-tumour drug against UDP-UGT’s. CK0403 is repor

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4

Othman, Salem, and Maria Kozurkova. "Sulfur Containing Acridine Derivatives in Preclinical Studies with Cancer Cell Lines." Current Medicinal Chemistry 25, no. 17 (2018): 1968–75. http://dx.doi.org/10.2174/0929867324666170414165019.

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Background: The possible use of acridines as anticancer agents was first considered in the 1920´s. Since then, a large number of acridine drugs have been tested as antitumour agents, including compounds containing sulphur on the acridine chromophore. In this review, we will discuss recent studies which have investigated the anticancer activity of this class of acridine derivatives. Methods: We present the results both of our own decade-long research and also of existing research literature into the anticancer activity of acridine derivatives containing sulphur. The evidence of specific tumor-c

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5

Gabriel, Iwona. "‘Acridines’ as New Horizons in Antifungal Treatment." Molecules 25, no. 7 (2020): 1480. http://dx.doi.org/10.3390/molecules25071480.

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Frequent fungal infections in immunocompromised patients and mortality due to invasive mycosis are important clinical problems. Opportunistic pathogenic Candida species remain one of the leading causes of systemic mycosis worldwide. The repertoire of antifungal chemotherapeutic agents is very limited. Although new antifungal drugs such as lanosterol 14α-demethylase and β-glucan synthase inhibitors have been introduced into clinical practice, the development of multidrug resistance has become increasingly significant. The urgency to expand the range of therapeutic options for the treatment of f

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6

Magesh M and Gandhimathi R. "An overview of pharmacological activities of acridine derivatives." International Journal of Research in Pharmaceutical Sciences 11, no. 4 (2020): 6922–31. http://dx.doi.org/10.26452/ijrps.v11i4.3683.

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The derivatives of acridine can be served as a lead molecule of an antibacterial, anti-viral antiprotozoal, anti-viral, antitubercular, anti-fungal, anti-malarial and anti-cancer agents. Even though the usage of acridine becomes limited due to its side effects, so many potent and safe compounds can be derived through molecular modification in the acridine ring. Since the resistance of pathogens and tumour cells has become more common nowadays, it necessitates the search of new drug candidates. Since the treatment and management of Alzheimer's disease is such a complicated and proper drug regim

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7

SANTANU, BHATTACHARYA, and THOMAS MINI. "DNA Binding Properties of Some Cationic Acridine Derivatives." Journal of Indian Chemical Society Vol. 75, Oct-Dec 1998 (1998): 716–24. https://doi.org/10.5281/zenodo.5917140.

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Department of Organic Chemistry, Indian Institute of Science, Bangalore-560 012<strong> </strong> <em>Manuscript received 17 August 1998</em> Four cationic acridine derivatives have been synthesized. The positively charged amine residue in one of these is connected directly on to the acridine nucleus and in three other acridines, the amines are connected via a 9-CH<sub>2</sub> unit to acridine. We have investigated the binding of these acridines with mammalian DNA by absorption titration, UV- and induced-CD spectroscopy and competitive ethidium bromide displacement fluorescence assay. The effe

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8

Galy, Jean-Pierre, Sandrine Morel, Gérard Boyer, and José Elguero. "Tetracyclic derivatives of acridine. Heterofused acridines." Journal of Heterocyclic Chemistry 33, no. 6 (1996): 1551–60. http://dx.doi.org/10.1002/jhet.5570330601.

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9

Rádl, Stanislav. "Preparation of 1-Hydroxyxanthen-9(9H)-ones and 1-Hydroxyacridin-9(10H)-ones via Corresponding 3,4-Dihydro-1,9(2H)-diones." Collection of Czechoslovak Chemical Communications 60, no. 12 (1995): 2127–36. http://dx.doi.org/10.1135/cccc19952127.

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Target 10-cyclopropyl-7-fluoro-1-hydroxy-6-(4-methyl-1-piperazinyl)acridin-9(10H)-one (IVc) and 7-fluoro-1-hydroxy-6-(4-methyl-1-piperazinyl)-9H-xanthen-9-one (IVd) were obtained from corresponding difluoro derivatives IVa and IVb, respectively. These intermediates were synthesized via respective 3,4-dihydro-1,9(2H)-diones Va and Vb. Acridine derivative (10-cyclopropyl-6,7-difluoro-3,4-dihydro-1H-acridine-1,9(2H,10H)-dione, Va) was synthesized from 1-cyclopropyl-6,7-difluoroisatoic anhydride (XI) and xanthene derivative (6,7-difluoro-3,4-dihydro-1H-xanthen-1,9(2H)-dione, Vb) from cyclohexenone

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10

Krochtová, Kristína, Annamária Halečková, Ladislav Janovec, Michaela Blizniaková, Katarína Kušnírová, and Mária Kožurková. "Novel 3,9-Disubstituted Acridines with Strong Inhibition Activity against Topoisomerase I: Synthesis, Biological Evaluation and Molecular Docking Study." Molecules 28, no. 3 (2023): 1308. http://dx.doi.org/10.3390/molecules28031308.

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A series of novel 3,9-disubstituted acridines were synthesized and their biological potential was investigated. The synthetic plan consists of eight reaction steps, which produce the final products, derivatives 17a–17j, in a moderate yield. The principles of cheminformatics and computational chemistry were applied in order to study the relationship between the physicochemical properties of the 3,9-disubstituted acridines and their biological activity at a cellular and molecular level. The selected 3,9-disubstituted acridine derivatives were studied in the presence of DNA using spectroscopic (U

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11

Konopa, Jerzy. "Antitumor acridines with diaminoalkylo pharmacophoric group." Pure and Applied Chemistry 73, no. 9 (2001): 1421–28. http://dx.doi.org/10.1351/pac200173091421.

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The substitution of acridine molecule in positions 1 and/or 4 with diaminoalkylo residue may result in obtaining derivatives displaying antitumor activity. The diaminoalkylo residue can be attached to acridine either directly or indirectly as a carboxamido moiety. In the former case, the presence of appropriate substituent in position para to diaminoalkylo residue is crucial for antitumor activity. Also, heterocyclic aromatic rings condensed with the acridine core can be considered as such substituents. Additional substituents introduced into the acridine core, especially those that may be tra

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12

Goni, Lipiar K. M. O., Mohammad A. Jafar Mazumder, Divya B. Tripathy, and Mumtaz A. Quraishi. "Acridine and Its Derivatives: Synthesis, Biological, and Anticorrosion Properties." Materials 15, no. 21 (2022): 7560. http://dx.doi.org/10.3390/ma15217560.

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The phenomenon of corrosion threatens metallic components, human safety, and the economy. Despite being eco-friendly and promising as a corrosion inhibitor, acridine has not been explored to its full potential. In this review, we have discussed multiple biological activities that acridines have been found to show in a bid to prove that they are environmentally benign and much less toxic than many inhibitors. Some synthetic routes to acridines and substituted acridines have also been discussed. Thereafter, a multitude of acridines and substituted acridines as corrosion inhibitors of different m

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13

Bender, Matthias, and Jens Christoffers. "Investigations into the Regioselectivity of Fischer Indole and Friedländer Quinoline Syntheses with Octahydroisobenzofuran and Octahydroisoindole Derivatives." Zeitschrift für Naturforschung B 66, no. 12 (2011): 1209–18. http://dx.doi.org/10.1515/znb-2011-1203.

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A Fischer indole synthesis with a cis-configurated octahydroisobenzofuran-6-one yielded exclusively a furo[3,4-c]carbazole derivative as the product of a regioselective angular annulation reaction. A Friedländer quinoline synthesis from the same substrate gave a mixture of angular and linear annulation products, i. e. furo[3,4-a]acridine and furo[3,4-b]acridine derivatives. When submitting a mixture of cis- and trans-octahydroisoindole derivatives to Fischer and Friedländer syntheses, the trans-starting material gave regioselectively linear annulation products, i. e. pyrrolo[3,4-b]carbazole an

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14

GALY, J. P., S. MOREL, G. BOYER, and J. ELGUERO. "ChemInform Abstract: Tetracyclic Derivatives of Acridine. Heterofused Acridines." ChemInform 28, no. 24 (2010): no. http://dx.doi.org/10.1002/chin.199724290.

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15

Tot, Miklos, Dejan Opsenica, Milena Mitric, et al. "New 9-aminoacridine derivatives as inhibitors of Botulinum neurotoxins and P. falciparum malaria." Journal of the Serbian Chemical Society 78, no. 12 (2013): 1847–64. http://dx.doi.org/10.2298/jsc130924112t.

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Steroidal and adamantane aminoacridine derivatives were prepared and tested as both botulinum neurotoxin (BoNT) inhibitors and antimalarials. Steroid-bound acridines provided good potency against both the BoNT/A and BoNT/B light chains (LCs). The observed inhibition of the BoNT/B LC by ca. 50% is the highest attained inhibitory activity against this serotype by acridine-based compounds to date. With respect to antimalarial activity, adamantane acridines were the most potent derivatives (IC50 = 6-9 nM, SI > 326), indicating that an adamantyl group is a better carries than a steroidal motif f

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16

Sonawane, Amol D., Dinesh R. Garud, Taro Udagawa, Yasuhiro Kubota, and Mamoru Koketsu. "Synthesis of thieno[2,3-c]acridine and furo[2,3-c]acridine derivatives via an iodocyclization reaction and their fluorescence properties and DFT mechanistic studies." New Journal of Chemistry 42, no. 18 (2018): 15315–24. http://dx.doi.org/10.1039/c8nj03511c.

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In this paper, we report the novel synthesis of thieno[2,3-c]acridine and furo[2,3-c]acridine derivatives via intramolecular iodocyclization reaction. The thieno[2,3-c]acridine derivatives exhibited blue fluorescence in hexane.

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17

Němcová, Irena, Karel Nesměrák, Božena Kafková, and Jan Sejbal. "Physicochemical Properties of 9-(Alkylsulfanyl)- and 9-(Arylsulfanyl)acridine Derivatives and Their Interaction with (2-Hydroxypropyl)cyclodextrins." Collection of Czechoslovak Chemical Communications 71, no. 2 (2006): 179–89. http://dx.doi.org/10.1135/cccc20060179.

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Acid-base properties and aggregations of 9-(alkylsulfanyl)- and 9-(arylsulfanyl)acridine derivatives were studied as a part of systematic study of physicochemical properties of these compounds synthesized as potential drugs. The effect of the (2-hydroxypropyl)cyclodextrins on these properties and their association with the acridines was also followed.

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18

Othman, Layla Ahmed. "THE GREEN APPROACH FOR THE SYNTHESIS OF SOME HYDROQUINOLINE DERIVATIVES COMPOUND VIA HANTZSCH REACTION." Science Journal of University of Zakho 12, no. 4 (2024): 428–36. http://dx.doi.org/10.25271/sjuoz.2024.12.4.1377.

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Since that hydroquinoline and acridine compounds serve as the fundamental building blocks for the synthesis of many different pharmaceuticals, they are among the most significant classes of chemical compounds that attract the interest of numerous researchers and pharmacologists. Therefore, in this research, The Hantzch reaction was used to prepare these types hydroquinoline and acridine derivatives of compounds, through the reaction of a number substituted benzaldehyde with demidone and α-β diketone substitutes by refluxed with sodium acetate in the presence of iodine and a 1-sulfo-4-(3-(Ferri

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19

Yang, Songjie, Jonathan C. Bristow, Matthew A. Addicoat, and John D. Wallis. "One step conversion of 1,5-bis(dimethylamino)naphthalene to salts of “back to back” bis-acridine derivatives." New Journal of Chemistry 44, no. 23 (2020): 9621–25. http://dx.doi.org/10.1039/d0nj00757a.

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1,5-Bis(dimethylamino)naphthalene can be oxidized directly to a dication or a cation derived from an acridino-acridine, the former stabilised by two dimethyliminium substituents, while the latter has a dimethylated nitrogen in the ring system.

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20

Albino, Sonaly, Michelangela Nobre, Jamire da Silva, et al. "Synthesis, Biological Evaluation, Molecular Dynamics, and QM-MM Calculation of Spiro-Acridine Derivatives Against Leishmaniasis." Microorganisms 13, no. 6 (2025): 1297. https://doi.org/10.3390/microorganisms13061297.

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Leishmaniasis is a neglected tropical disease caused by Leishmania sp. The therapeutic arsenal is reduced and limited. In this context, acridine derivatives present themselves as promising leishmanicidal compounds. This paper involved synthesizing and evaluating the antileishmanial and immunomodulatory potential of spiro-acridine derivatives. Six spiro-acridine derivatives were obtained through nucleophilic substitution reactions between the acetohydrazide/acetamide intermediates and 9-carbaldehydeacridine, followed by spontaneous cyclization. IR, NMR, and HRMS confirmed the structures. These

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21

Di Giorgio, Carole, Florence Delmas, Nathalie Filloux, et al. "In Vitro Activities of 7-Substituted 9-Chloro and 9-Amino-2-Methoxyacridines and Their Bis- and Tetra-Acridine Complexes against Leishmania infantum." Antimicrobial Agents and Chemotherapy 47, no. 1 (2003): 174–80. http://dx.doi.org/10.1128/aac.47.1.174-180.2003.

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ABSTRACT 9-Chloro and 9-amino-2-methoxyacridines bearing different substituents in position 7, as well as their corresponding unsubstituted dimeric and tetrameric complexes, were investigated for in vitro antiproliferative properties against Leishmania infantum compared to toxicity towards human monocytes. The results clearly confirmed that several compounds of the 2-methoxyacridine series, together with their corresponding dimeric and tetrameric derivatives, had strong in vitro antiparasitic properties. Antileishmanial activity was shown to depend on the nature of both 7- and 9-substituted gr

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22

Rak, Janusz, Karol Krzyminski, Piotr Skurski, et al. "X-Ray, Quantum Mechanics and Density Functional Methods in the Examination of Structure and Tautomerism of N-Methyl-Substituted Acridin-9-amine Derivatives." Australian Journal of Chemistry 51, no. 8 (1998): 643. http://dx.doi.org/10.1071/c97205.

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X-Ray diffraction has shown that N,N-dimethylacridin-9-amine (4) and N ,10-dimethylacridin-9-imine (5) both crystallize in the monoclinic space group P21/c (No. 14) with four molecules in the unit cell. The dimethylamino group in (4) is twisted through an angle of 58·6° relative to a nearly planar acridine moiety. On the other hand, the central ring in (5) is folded along the C(9) · · · N(10) axis through an angle of 26·3° and the exocyclic nitrogen atom with the methyl group attached to it is directed away from the concave side of the acridine nucleus. Theoretical ab initio Hartree–Fock (HF)

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23

Farat, Oleg, Svetlana Varenichenko, Victor Markov, and Karolina Yanova. "IN SILICO PREDICTION OF BIOLOGICAL ACTIVITY OF BROMO DERIVATIVES OF HYDROACRIDINES." Ukrainian Chemistry Journal 89, no. 6 (2023): 97–110. http://dx.doi.org/10.33609/2708-129x.89.06.2023.97-110.

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The aim of the work was to establish the spectrum of biological activity of new derivatives of 9-bromo-1,2,3,4-tetrahydroacridine due to the limited amount of literature data. In silico prediction of selected bromo-derivatives of hydrogenated acridines was performed using the SuperPred 3.0 web resource. The obtained results were compared with the results of prediction of active drugs that contain the acridine cycle in their structure - Tacrine, Amiridine and Amsacrine. Results ≤80% were taken into account. The most promising compound was 9-bromo-1,2,3,4-tetrahydroacridine. A common predict

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24

Zhu, Shangrong, Xuechen Lu, Qiuneng Xu, Jian Li, and Shenghu Yan. "Cu-Catalyzed Cascade Reaction of Isoxazoles with Diaryliodonium Salts for the Synthesis of Acridines." Letters in Organic Chemistry 17, no. 12 (2020): 944–50. http://dx.doi.org/10.2174/1570178617666200225125427.

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A straightforward and efficient synthesis of acridine derivatives via a copper-catalyzed cascade reaction among isoxazoles and diaryliodonium salts is achieved. Various mono-, multi-substituted and 9-substituted acridine derivatives could be obtained in moderate to good yields. The process has gone through tandem double arylation and Friedel-Crafts reactions.

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25

Vilková, Mária, Monika Hudáčová, Nikola Palušeková, et al. "Acridine Based N-Acylhydrazone Derivatives as Potential Anticancer Agents: Synthesis, Characterization and ctDNA/HSA Spectroscopic Binding Properties." Molecules 27, no. 9 (2022): 2883. http://dx.doi.org/10.3390/molecules27092883.

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A series of novel acridine N-acylhydrazone derivatives have been synthesized as potential topoisomerase I/II inhibitors, and their binding (calf thymus DNA—ctDNA and human serum albumin—HSA) and biological activities as potential anticancer agents on proliferation of A549 and CCD-18Co have been evaluated. The acridine-DNA complex 3b (-F) displayed the highest Kb value (Kb = 3.18 × 103 M−1). The HSA-derivatives interactions were studied by fluorescence quenching spectra. This method was used for the calculation of characteristic binding parameters. In the presence of warfarin, the binding const

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26

Karelou, Maria, Vasileios Kourafalos, Athanasia P. Tragomalou, et al. "Synthesis, Biological Evaluation and Stability Studies of Some Novel Aza-Acridine Aminoderivatives." Molecules 25, no. 19 (2020): 4584. http://dx.doi.org/10.3390/molecules25194584.

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Several new amino-substituted aza-acridine derivatives bearing a basic side chain have been designed and synthesized. The antiproliferative activity of the target compounds has been evaluated against three cancer cell lines—namely HCT-116 (colorectal), the uterine sarcoma MES-SA, and its doxorubicin-resistant variant MES-SA/Dx5. A limited number of the new acridines showed marginal cytotoxicity against the tested cell lines; nevertheless, these analogues possessed a similar substitution pattern. The moderate biological activity of these derivatives was attributed to their instability in aqueou

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27

Tomaščiková, Jana, Ján Imrich, Ivan Danihel, Stanislav Böhm, and Pavol Kristian. "Heterocyclization of (Acridin-9-yl)thiosemicarbazides with Dimethyl Acetylenedicarboxylate." Collection of Czechoslovak Chemical Communications 72, no. 3 (2007): 347–62. http://dx.doi.org/10.1135/cccc20070347.

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Two types of (acridin-9-yl)thiosemicarbazides with the acridine moiety in the thiourea part (Acr-NHCS, 10a, 10b) and hydrazine part (Acr-NHNHCS, 12a-12c) were prepared to investigate their reactions with dimethyl acetylenedicarboxylate. Five-membered thiazolidinone derivatives 15a, 15b, 19a-19c were formed; some aspects of corresponding reaction mechanisms are discussed. 1D and 2D 1H and 13C NMR spectroscopy and DFT quantum chemical calculations were used to elucidate the structure of the compounds.

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28

Dzierzbicka, K., M. Gozdowska, P. Sowiński, B. Wysocka-Skrzela, and A. M. Kołodziejczyk. "NMR studies of the MDP conjugates with amino-acridine/acridone derivatives." Letters in Peptide Science 5, no. 5-6 (1998): 409–12. http://dx.doi.org/10.1007/bf02443496.

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29

Chen, Rui, Lini Huo, Yogini Jaiswal, et al. "Design, Synthesis, Antimicrobial, and Anticancer Activities of Acridine Thiosemicarbazides Derivatives." Molecules 24, no. 11 (2019): 2065. http://dx.doi.org/10.3390/molecules24112065.

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Background: Acridine and thiourea derivatives are important compounds in medicinal chemistry due to their diverse biological properties including anticancer and antimicrobial effects. However, literature reveals some side effects associated with use of acridines. It is suggested that hybrid molecules may reduce the side effects and enhance the beneficial properties due to synergistic activity. The objectives of the present study are to synthesize and evaluate the anticancer and antimicrobial properties of new hybrids of acridine thiosemicarbazides derivatives. Results: The structures of the sy

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30

Denny, William. "Chemotherapeutic Effects of Acridine Derivatives." Medicinal Chemistry Reviews - Online 1, no. 3 (2004): 257–66. http://dx.doi.org/10.2174/1567203043401923.

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31

Gazova, Zuzana, Andrea Bellova, Zuzana Daxnerova, et al. "Acridine derivatives inhibit lysozyme aggregation." European Biophysics Journal 37, no. 7 (2008): 1261–70. http://dx.doi.org/10.1007/s00249-008-0313-0.

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32

Piestrzeniewicz, Mariola K., Dorota Wilmańska, Kazimierz Studzian, et al. "Inhibition of RNA Synthesis in vitro by Acridines - Relation between Structure and Activity." Zeitschrift für Naturforschung C 53, no. 5-6 (1998): 359–68. http://dx.doi.org/10.1515/znc-1998-5-610.

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Abstract The effects of acridine derivatives (proflavine and 2,7-dialkyl derivatives, diacridines and triacridines, 9-aminoacridine carboxamides, and 9-anilinoacridine, amsacrine and its congeners) on overall RNA synthesis in vitro, on synthesis of initiating oligonucleotides and the binding of the enzyme to DNA were studied. The primary mechanism of action is related to inhibition of the enzyme binding to DNA. The acridines (intercalating or non-intercalating and bis-intercalating ligands) assayed here differ in the properties of their complexes with DNA. Correlation is generally observed bet

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33

Druzina, Anna A., Nadezhda V. Dudarova, Ivan V. Ananyev, et al. "New Boron Containing Acridines: Synthesis and Preliminary Biological Study." Molecules 28, no. 18 (2023): 6636. http://dx.doi.org/10.3390/molecules28186636.

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The synthesis of the first conjugates of acridine with cobalt bis(dicarbollide) are reported. A novel 9-azido derivative of acridine was prepared through the reaction of 9-methoxyacridine with N3CH2CH2NH2, and its solid-state molecular structure was determined via single-crystal X-ray diffraction. The azidoacridine was used in a copper (I)-catalyzed azide-alkyne cycloaddition reaction with cobalt bis(dicarbollide)-based terminal alkynes to give the target 1,2,3-triazoles. DNA interaction studies via absorbance spectroscopy showed the weak binding of the obtained conjugates with DNA. The antipr

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34

Shchepochkin, A. V., A. F. Uglova, I. A. Utepova, et al. "AMINO DERIVATIVES OF ACRIDINE: SYNTHESIS, STUDY OF ANTICHOLINESTERASE AND ANTIOXIDANT ACTIVITIES." Доклады Российской академии наук. Химия, науки о материалах 509, no. 1 (2023): 34–40. http://dx.doi.org/10.31857/s268695352370019x.

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A simple and accessible approach to the synthesis of new amine derivatives of acridine based on the direct C–H functionalization methodology was developed. The inhibitory effect of the synthesized compounds on cholinesterases and carboxylesterases, as well as their antioxidant activity, was studied. A moderate inhibition of BChE by the morpholine and pyrazole derivatives of acridine and a high anti-BChE activity of the N-methyl-piperazine one were shown.

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35

Gensicka-Kowalewska, Monika, Mirosława Cichorek, Anna Ronowska, Milena Deptuła, Ilona Klejbor, and Krystyna Dzierzbicka. "Synthesis and Biological Evaluation of Acridine/Acridone Analogs as Potential Anticancer Agents." Medicinal Chemistry 15, no. 7 (2019): 729–37. http://dx.doi.org/10.2174/1573406414666181015145120.

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Background: The lack of efficacious therapy for advanced melanoma and neuroblastoma makes new approaches necessary. Therefore, many scientists seek new, more effective, more selective and less toxic anticancer drugs. Objective: We propose the synthesis of the new functionalized analogs of 1-nitroacridine/4- nitroacridone connected to tuftsin/retro-tuftsin derivatives as potential anticancer agents. Methods: Acridine and acridone analogues were prepared by Ullmann condensation and then cyclization reaction. As a result of nucleophilic substitution reaction 1-nitro-9-phenoxyacridine or 1- chloro

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Garberová, Monika, Ivan Potočňák, Monika Tvrdoňová, et al. "Derivatives Incorporating Acridine, Pyrrole, and Thiazolidine Rings as Promising Antitumor Agents." Molecules 28, no. 18 (2023): 6616. http://dx.doi.org/10.3390/molecules28186616.

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Derivatives combining acridine, pyrrole, and thiazolidine rings have emerged as promising candidates in the field of antitumor drug discovery. This paper aims to highlight the importance of these three structural motifs in developing potent and selective anticancer agents. The integration of these rings within a single molecule offers the potential for synergistic effects, targeting multiple pathways involved in tumor growth and progression. Spiro derivatives were efficiently synthesized in a two-step process starting from isothiocyanates and 2-cyanoacetohydrazide. The thiourea side chain in s

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Zhang, Qing, Shuaiqiang Sun, Won Jae Chung, et al. "Highly efficient TADF OLEDs with low efficiency roll-off based on novel acridine–carbazole hybrid donor-substituted pyrimidine derivatives." Journal of Materials Chemistry C 7, no. 39 (2019): 12248–55. http://dx.doi.org/10.1039/c9tc04284a.

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Dimethyl acridine (Ac) and carbazole (Cz) donors are fused to produce acridine–carbazole hybrid donors 12AcCz (8,8-dimethyl-5-phenyl-8,13-dihydro-5H-indolo[2,3-c]acridine) and 23AcCz (13,13-dimethyl-7-phenyl-7,13-dihydro-5H-indolo[3,2-b]acridine).

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Herole RA, Rakesh Kumar Jat, and Rajendra D Dighe. "A REVIEW ON ACRIDINE, XANTHENE AND ITS DERIVATIVES: SYNTHESIS, PHYSICAL AND PHARMACOLOGICAL PROPERTIES." Tropical Journal of Pharmaceutical and Life Sciences 9, no. 6 (2022): 01–12. https://doi.org/10.61280/tjpls.v9i6.108.

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Acridine derivatives are one of the oldest category of bioactive, globally used as anticancer, antiprotozoal agents and antibacterial. The class of acridine derivatives constitutes an interesting group of nitrogen-containing tricyclic compounds that caught the scientific group’s attention, mainly due to its wide range of pharmaceutical properties. The synthesis of new polycyclic acridine skeletons fused with a five or six-membered rings, have been extensively studied because they play important roles in some DNA-intercalating anticancer drugs. Benzoacridine derivatives have been recently synth

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Herole R A and Rakesh Kumar Jat. "Synthesis, Characterisation and Anticancer Study of Acridine derivatives." Tropical Journal of Pharmaceutical and Life Sciences 10, no. 5 (2023): 50–56. http://dx.doi.org/10.61280/tjpls.v10i5.146.

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Cancer is one of the global problem and a major cause for mortality. many treatment strategies are available for cancer treatment, still there is a scope for novel treatment to avoid serious side effects of existing therapy. Novel DNA binding agents are needed for effective treatment of cancers. In the field of antitumor DNA-intercalating agents, 9-aminoacridines play an important role due to their antiproliferative properties. Several cancer chemotherapeutics such as amsacrine and nitracrine have been developed as anticancer agents.In present study, a series of new acridine-based derivatives

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Akishina, E. A., D. V. Kazak, Е. А. Dikusar, R. S. Alexeev, N. A. Bumagin, and V. I. Potkin. "Pyridine Derivatives of Acridine and Quinoline." Russian Journal of General Chemistry 90, no. 12 (2020): 2230–41. http://dx.doi.org/10.1134/s1070363220120038.

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Song, buer, Minghui Li, and Mukhtar Imerhasan. "Synthesis and Application of Acridine Derivatives." Chinese Journal of Organic Chemistry 38, no. 3 (2018): 594. http://dx.doi.org/10.6023/cjoc201710007.

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Tonelli, Michele, Gerolamo Vettoretti, Bruno Tasso, et al. "Acridine derivatives as anti-BVDV agents." Antiviral Research 91, no. 2 (2011): 133–41. http://dx.doi.org/10.1016/j.antiviral.2011.05.005.

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Szymanska, A., W. Wiczk, and L. Lankiewicz. "Synthesis and photophysics of acridine derivatives." Chemistry of Heterocyclic Compounds 36, no. 7 (2000): 801–8. http://dx.doi.org/10.1007/bf02256913.

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Ishihara, Yoshimi, Takeyuki Ito, Hiroshi Saito, and Jiro Takano. "Reaction of acridine with pyrazolone derivatives." Journal of Heterocyclic Chemistry 42, no. 5 (2005): 963–67. http://dx.doi.org/10.1002/jhet.5570420533.

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Brown, CL, MM Harding, GY Krippner, S. Rainone, and LK Webster. "Preparation and Biological Activity of Heteroaryl-Substituted Bile Steroids." Australian Journal of Chemistry 49, no. 1 (1996): 7. http://dx.doi.org/10.1071/ch9960007.

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The synthesis, and growth inhibition studies against the L1210 mouse leukaemia, �MCF-7 human breast cancer and SKOV-3 ovarian carcinoma cell lines, of derivatives of lithocholic acid and cholic acid in which quinoline-3-carboxylate and acridine-9-carboxylate are substituted at the 3 and/or the 24 position are reported. The 3α,24-diheteroaryl-substituted steroid systems, lithocholic acid, cholic acid, quinoline and acridine-9-carboxylic acid showed no significant biological activity against any of the cell lines. In contrast, when either a single quinoline-3-carboxylate or acridine-9-carboxylat

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Lantsova, A. V., E. V. Sanarova, L. L. Nikolaeva, et al. "Development of a model of a dosage form for a new domestic compound (pyrrolo[3,2-l]acridinone derivative) and studying its cytotoxic activity." Russian Journal of Biotherapy 23, no. 3 (2024): 57–64. http://dx.doi.org/10.17650/1726-9784-2024-23-3-57-64.

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Background. Expanding the list of safe and effective medicines are the main directions of development of modern medicine and pharmacy. Acridine derivatives are an interesting object of study due to their proven antitumor effect on leukemia and lymphoma. The mechanism of their antitumor effect is the ability to intercalate DNA, as well as to inhibit topoisomerases and telomerase, initiate ROS-mediated oxidative stress, arrest the cell cycle, and interact with glycoprotein-P.Aim. To develop the composition and technology for obtaining a model pharmaceutical form (PF) for parenteral use of a new

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Chen, Minyu, Jiali Yang, Zhonghua Ye, et al. "Extremely low-efficiency roll-off of phosphorescent organic light-emitting diodes at high brightness based on acridine heterocyclic derivatives." Journal of Materials Chemistry C 6, no. 36 (2018): 9713–22. http://dx.doi.org/10.1039/c8tc02739k.

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Ghosh, Subhajit, Tapas Das, Shishu K. Suman, Haladhar D. Sarma, and Ashutosh Dash. "Preparation and Preliminary Evaluation of 68 Ga-Acridine: An Attempt to Study the Potential of Radiolabeled DNA Intercalator as a PET Radiotracer for Tumor Imaging." Anti-Cancer Agents in Medicinal Chemistry 20, no. 13 (2020): 1538–47. http://dx.doi.org/10.2174/1871520620666200502002609.

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Introduction: Acridine is a well-known DNA intercalator and thereby gets easily inserted within DNA. As uncontrolled rapid cell division is one of the primary characteristics of the tumors, it is expected that acridine or its suitable derivatives will have preferential accumulation in the tumorous lesions. Therefore, an attempt was made to radiolabel an acridine derivative with 68Ga and study the potential of the 68Ga-acridine complex as a PET agent for tumor imaging. Methods: 9-aminoacridine was coupled with p-NCS-benzyl-DOTA to render it suitable for labeling with 68Ga. The purified acridine

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Antonini, Ippolito. "Intriguing Classes of Acridine Derivatives as DNA-binding Antitumour Agents: From Pyrimido[5,6,1-de]acridines to Bis(acridine-4-carboxamides)." Medicinal Chemistry Reviews - Online 1, no. 3 (2004): 267–90. http://dx.doi.org/10.2174/1567203043401851.

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Belmont, Philippe, Johann Bosson, Thomas Godet, and Martin Tiano. "Acridine and Acridone Derivatives, Anticancer Properties and Synthetic Methods: Where Are We Now?" Anti-Cancer Agents in Medicinal Chemistry 7, no. 2 (2007): 139–69. http://dx.doi.org/10.2174/187152007780058669.

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