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

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

Volume: 8 Issue: 3

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

Affiliation:

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

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.

Cite this article as:

Dundar Yasemin, Ozatik Yasemin, Ozatik Orhan, Ergin Volkan, Onkol Tijen, Menevse Adnan, Erol Kevser and Fethi Sahin M., Synthesis and Biological Evaluation of the Salicylamide and Salicylic Acid Derivatives as Anti-Estrogen Agents, Medicinal Chemistry 2012; 8 (3) . https://dx.doi.org/10.2174/1573406411208030481