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Design, synthesis, docking study and cytotoxic activity evaluation of some novel letrozole analogs.


ABSTRACT: Breast cancer is the most common type of female cancer. One class of hormonal therapy for breast cancer drugs -non steroidal aromatase inhibitors- are triazole analogues. In this work, some derivatives of these drugs was designed and synthesized. All synthesized compounds were evaluated for their cytotoxic activities on breast cancer cell lines (MDA-MB-231, T47D and MCF-7).Our synthetic route for designed compounds started from 4-bromotolunitrile which was reacted with 1H-1,2,4-triazole to afford 4-(4-cyanobenzyl)-1,2,4-triazole. The reaction of later compound with aromatic aldehydes led to formation of the designed compounds. Eleven novel derivatives 1a-k were tested for their cytotoxic activities on three human breast cancer cell lines.Among the synthesized compound, 4-[2-(3-chlorophenyl)-1-(1H-1,2,4-triazol-1-yl)ethenyl]benzonitrile (1c) showed the highest activity against MCF-7 and MDA-MB-231 cell lines and 4-[2-(4-methoxyphenyl)-1-(1H-1,2,4-triazol-1-yl)ethenyl]benzonitrile (1 h) exhibited highest activity against T47D cell line. According to cytotoxic activities results, compound 4-[2-(4-dimethylamino)-1-(1H-1,2,4-triazol-1-yl)ethenyl]benzonitrile (1 k) showed comparative activity against T47D and MDA-MB-231 cell lines with compound (1 h) and our reference drug Etoposide.In the process of anti-cancer drug discovery, to find new potential anti-breast cancer agents, we designed and synthesized a novel series of letrozole analogs. Cytotoxicity evaluation revealed that compounds (1c) and (1 k) were the most potent compounds with comparative activity with Etoposide. The results revealed that ?-? interactions are responsible for the enzyme inhibitions of compounds (1 c) and (1 k).

SUBMITTER: Vosooghi M 

PROVIDER: S-EPMC4284924 | biostudies-literature | 2014 Dec

REPOSITORIES: biostudies-literature

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Design, synthesis, docking study and cytotoxic activity evaluation of some novel letrozole analogs.

Vosooghi Mohsen M   Firoozpour Loghman L   Rodaki Abolfazl A   Pordeli Mahboobeh M   Safavi Maliheh M   Ardestani Sussan K SK   Dadgar Armin A   Asadipour Ali A   Moshafi Mohammad Hassan MH   Foroumadi Alireza A  

Daru : journal of Faculty of Pharmacy, Tehran University of Medical Sciences 20141224


<h4>Background</h4>Breast cancer is the most common type of female cancer. One class of hormonal therapy for breast cancer drugs -non steroidal aromatase inhibitors- are triazole analogues. In this work, some derivatives of these drugs was designed and synthesized. All synthesized compounds were evaluated for their cytotoxic activities on breast cancer cell lines (MDA-MB-231, T47D and MCF-7).<h4>Methods</h4>Our synthetic route for designed compounds started from 4-bromotolunitrile which was reac  ...[more]

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