Some new quinolinederivatives were designed and synthesized to evaluate their biological activities as aromatase inhibitors andanti-breast cancer agents.Cytotoxicity of quinolines8a-g against human breast cancer MCF-7 and T47D cell lines wereevaluated. 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.Theireffectson Aromataseactivity are also described.Our results showed that compound 8b inhibits aromatase enzyme activity more than reference drug Letrozol.
Design, synthesis and biological evaluation of4-(Imidazolylmethyl)-2-aryl-quinoline derivatives as aromatase inhibitors and anti-breast cancer agents
FERLIN, MARIA GRAZIA;
2015
Abstract
Some new quinolinederivatives were designed and synthesized to evaluate their biological activities as aromatase inhibitors andanti-breast cancer agents.Cytotoxicity of quinolines8a-g against human breast cancer MCF-7 and T47D cell lines wereevaluated. 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.Theireffectson Aromataseactivity are also described.Our results showed that compound 8b inhibits aromatase enzyme activity more than reference drug Letrozol.
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