Synthesis and Biological Evaluation of the Salicylamide and Salicylic Acid Derivatives as Anti-Estrogen Agents
2012
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.
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