Medicinal Chemistry 2012-05-01

Synthesis and biological evaluation of the salicylamide and salicylic acid derivatives as anti-estrogen agents.

Yasemin Dündar, Yasemin Özatik, Orhan Özatik, Volkan Ergin, Tijen Önkol, Adnan Menevşe, Kevser Erol, M Fethi Sahin

文献索引：Med. Chem. 8(3) , 481-90, (2012)

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摘要

Alkylphenols have xenoestrogenic activity, which mimic the action of physiological estrogens and these mimicking activities are mainly mediated by nongenomic pathway. Nongenomic pathway plays a pivotal role in breast, endometrial and ovarian cancers' growth and development. In this study, various alkylphenol derivatives were prepared and screened for their anti-uterotrophic and uterotrophic activity. Among these compounds, 2-hydroxy-5-nonanoylbenzamide (compound 1b) showed 93.99% inhibitory activity in the anti-uterotrophic test performed, and was found inactive in the uterotrophic activity test. Moreover, all test compounds were examined for the effect on uterine histopathological changes, and plasma 17β-estradiol (E2) level. Compound 1b was also tested for in vitro anti-cancer activity against ER+, human breast cancer cell line MCF-7, and it reduced cell viability to 74.01% at 50 nM concentration.