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, Afshin Zarghi

Journal Name: Letters in Drug Design & Discovery

Volume 13 , Issue 1 , 2016

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Graphical 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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Article Details

Year: 2016
Published on: 11 June, 2015
Page: [89 - 97]
Pages: 9
DOI: 10.2174/1570180812666150611185605

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