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


DÜNDAR Y., ÖZATİK F. Y. , ÖZATİK O. , ERGİN V., ÖNKOL T., Menevşe A., ...More

MEDICINAL CHEMISTRY, vol.8, no.3, pp.481-490, 2012 (Journal Indexed in SCI) identifier identifier identifier

  • Publication Type: Article / Article
  • Volume: 8 Issue: 3
  • Publication Date: 2012
  • Doi Number: 10.2174/1573406411208030481
  • Title of Journal : MEDICINAL CHEMISTRY
  • Page Numbers: pp.481-490

Abstract

Alkylphenols have xenoestrogenic activity, which mimic the action of physiological estrogens and these mim-icking 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 17 beta-estradiol (E-2) 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.