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:Department of Pharmaceutical Chemistry, School of Pharmacy, Shahid Beheshti University of Medical Sciences, Tehran, Iran.
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.
