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

[ Vol. 8 , Issue. 3 ]

Author(s):

Yasemin Dundar, Yasemin Ozatik, Orhan Ozatik, Volkan Ergin, Tijen Onkol, Adnan Menevse, Kevser Erol and M. Fethi Sahin   Pages 481 - 490 ( 10 )

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

Affiliation:

Gazi University, Faculty of Pharmacy, Department of Pharmaceutical Chemistry, Tac Sk. 06330 Etiler, Ankara, Turkey.



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