Synthesis and Biological Evaluation of the Salicylamide and Salicylic Acid Derivatives as Anti-Estrogen Agents

Author(s): Yasemin Dundar, Yasemin Ozatik, Orhan Ozatik, Volkan Ergin, Tijen Onkol, Adnan Menevse, Kevser Erol, M. Fethi Sahin.

Journal Name: Medicinal Chemistry

Volume 8 , Issue 3 , 2012

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Abstract:

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.

Keywords: Anti-breast cancer activity, anti-estrogenic activity, anti-uterotrophic activity, nongenomic response, pnonylphenol, xenoestrogens, Alkylphenols, xenoestrogenic activity, nonanoylbenzamide, β-estradiol

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Article Details

VOLUME: 8
ISSUE: 3
Year: 2012
Page: [481 - 490]
Pages: 10
DOI: 10.2174/1573406411208030481
Price: $58

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