Generic placeholder image

Medicinal Chemistry

Editor-in-Chief

ISSN (Print): 1573-4064
ISSN (Online): 1875-6638

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 and M. Fethi Sahin

Volume 8, Issue 3, 2012

Page: [481 - 490] Pages: 10

DOI: 10.2174/1573406411208030481

Price: $65

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


Rights & Permissions Print Cite
© 2024 Bentham Science Publishers | Privacy Policy