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

作者：Ghodsi Razieh; Azizi Ebrahim; Ferlin Maria Grazia; Pezzi Vincenzo; Zarghi Afshin^*

来源：Letters in Drug Design and Discovery, 2016, 13(1): 89-97.

DOI：10.2174/1570180812666150611185605

• Aromatase activity
• breast cancer
• MCF-7
• quinolines
• T47D

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.

• 出版日期2016