Synthesis and antileishmanial activity of 6-mono-substituted and 3,6-di-substituted acridines obtained by acylation of proflavine

Giorgio, Carole Di; Shimi, Kamal; Boyer, G.; Delmas, F.; Galy, Jean

doi:10.1016/j.ejmech.2007.02.010

Cited by 59 publications

(32 citation statements)

References 16 publications

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“…Acridines have been used as antimicrobial [7,8], antiparasitic [9] and anticancer agents for many years and binding to DNA considered to be a principal mode of their bioactivity [10]. The best known acridine drug amsacrine [N-(4-(acridin-9-ylamino)-3-methoxyphenyl) methanesulfonamide] is routinely employed for systemic treatment of human cancers [11].…”

mentioning

confidence: 99%

Cytotoxic activity of acridin-3,6-diyl dithiourea hydrochlorides in human leukemia line HL-60 and resistant subline HL-60/ADR

Vantová

Paulíková

Sabolová³

et al. 2009

International Journal of Biological Macromolecules

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confidence: 99%

Cytotoxic activity of acridin-3,6-diyl dithiourea hydrochlorides in human leukemia line HL-60 and resistant subline HL-60/ADR

Vantová

Paulíková

Sabolová³

et al. 2009

International Journal of Biological Macromolecules

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“…We have payed special attention to quinoline, which constitutes the central nucleus of sitamaquine (25,26), acridine (27,28), quinoxaline (29)(30)(31), and coumarins (32,33). On the other hand, nitrofuran compounds (34,35), the most relevant registered as nifurtimox, and derivatives of the benzodioxol core (36) have been selected.…”

mentioning

confidence: 99%

Novel Heteroaryl Selenocyanates and Diselenides as Potent Antileishmanial Agents

Baquedano

Alcolea

Toro

et al. 2016

Antimicrob Agents Chemother

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A series of new selenocyanates and diselenides bearing interesting bioactive scaffolds (quinoline, quinoxaline, acridine, chromene, furane, isosazole, etc.) was synthesized, and their in vitro leishmanicidal activities against Leishmania infantum amastigotes along with their cytotoxicities in human THP-1 cells were determined. Interestingly, most tested compounds were active in the low micromolar range and led us to identify four lead compounds (1h, 2d, 2e, and 2f) with 50% effective dose (ED 50 ) values ranging from 0.45 to 1.27 M and selectivity indexes of >25 for all of them, much higher than those observed for the reference drugs. These active derivatives were evaluated against infected macrophages, and in order to gain preliminary knowledge about their possible mechanism of action, the inhibition of trypanothione reductase (TryR) was measured. Among these novel structures, compounds 1h (3,5-dimethyl-4-isoxazolyl selenocyanate) and 2d [3,3=-(diselenodiyldimethanediyl)bis(2-bromothiophene)] exhibited good association between TryR inhibitory activity and antileishmanial potency, pointing to 1h, for its excellent theoretical ADME (absorption, distribution, metabolism, and excretion) properties, as the most promising lead molecule for leishmancidal drug design.

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“…Acridine derivatives possess a diverse range of pharmacological activities [14–16]. Hence all the chalcone and isoxazole-substituted 9-anilino acridine derivatives 4a–j, 5a–j were screened for antioxidant activity and short-term in vitro antitumor activity against Daltons Lymphoma Ascites (DLAs) cells.…”

Section: Biological Evaluationmentioning

confidence: 99%

Docking Studies, Synthesis, Characterization and Evaluation of Their Antioxidant and Cytotoxic Activities of Some Novel Isoxazole-Substituted 9-Anilinoacridine Derivatives

Rajagopal

Rafick

Sankar

et al. 2012

The Scientific World Journal

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A convenient synthesis of novel isoxazole-substituted 9-anilinoacridine derivatives 5a–j was reported. The compounds were confirmed by physical and analytical data and screened for in vitro antioxidant activity by DPPH method, reducing power assay and total antioxidant capacity method. The cytotoxic activity of the compounds was also studied in HEp-2 cell line. The docking studies of the synthesized compounds were performed towards the key nucleoside dsDNA by using AutoDock vina 4.0 programme. All the isoxazole-substituted compounds have significant activities.

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Synthesis and antileishmanial activity of 6-mono-substituted and 3,6-di-substituted acridines obtained by acylation of proflavine

Cited by 59 publications

References 16 publications

Cytotoxic activity of acridin-3,6-diyl dithiourea hydrochlorides in human leukemia line HL-60 and resistant subline HL-60/ADR

Cytotoxic activity of acridin-3,6-diyl dithiourea hydrochlorides in human leukemia line HL-60 and resistant subline HL-60/ADR

Novel Heteroaryl Selenocyanates and Diselenides as Potent Antileishmanial Agents

Docking Studies, Synthesis, Characterization and Evaluation of Their Antioxidant and Cytotoxic Activities of Some Novel Isoxazole-Substituted 9-Anilinoacridine Derivatives

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