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Letters in Drug Design & Discovery

Editor-in-Chief

ISSN (Print): 1570-1808
ISSN (Online): 1875-628X

Design, Synthesis and Biological Evaluation of 4-(Imidazolylmethyl)-2- Aryl-Quinoline Derivatives as Aromatase Inhibitors and Anti-breast Cancer Agents

Author(s): Razieh Ghodsi, Ebrahim Azizi, Maria Grazia Ferlin, Vincenzo Pezzi and Afshin Zarghi

Volume 13, Issue 1, 2016

Page: [89 - 97] Pages: 9

DOI: 10.2174/1570180812666150611185605

Price: $65

Abstract

Some new quinoline derivatives were designed and synthesized to evaluate their biological activities as aromatase inhibitors and anti-breast cancer agents. Cytotoxicity of quinolines 8a-g against human breast cancer MCF-7 and T47D cell lines were evaluated. All the compounds 8a-g were more cytotoxic against MCF-7 cells in comparison with those of T47D which express aromatase mRNA less than MCF-7 cells. Their effects on Aromatase activity are also described. Our results showed that compound 8b inhibits aromatase enzyme activity more than reference drug Letrozol.

Keywords: Aromatase activity, breast cancer, MCF-7, quinolines, T47D.

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