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



Ghodsi R1 ; Azizi E2 ; Ferlin MG3 ; Pezzi V4 ; Zarghi A5
Authors

Source: Letters in Drug Design and Discovery Published:2016


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. © 2016 Bentham Science Publishers.
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