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

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

Volume: 13 Issue: 1

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

Affiliation:

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

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.

Cite this article as:

Ghodsi Razieh, Azizi Ebrahim, Grazia Ferlin Maria, Pezzi Vincenzo and Zarghi Afshin, Design, Synthesis and Biological Evaluation of 4-(Imidazolylmethyl)-2- Aryl-Quinoline Derivatives as Aromatase Inhibitors and Anti-breast Cancer Agents, Letters in Drug Design & Discovery 2016; 13 (1) . https://dx.doi.org/10.2174/1570180812666150611185605

DOI https://dx.doi.org/10.2174/1570180812666150611185605	Print ISSN 1570-1808
Publisher Name Bentham Science Publisher	Online ISSN 1875-628X