title: Synthesis and biological evaluation of the salicylamide and salicylic acid derivatives as anti-estrogen agents.
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.
authors.affiliation: Gazi University, Faculty of Pharmacy, Department of Pharmaceutical Chemistry, Taç Sk. 06330 Etiler, Ankara, Turkey. yasemina@gazi.edu.tr
authors.forename: Yasemin
authors.initials: Y
authors.lastname: Dündar
authors.forename: Yasemin
authors.initials: Y
authors.lastname: Özatik
authors.forename: Orhan
authors.initials: O
authors.lastname: Özatik
authors.forename: Volkan
authors.initials: V
authors.lastname: Ergin
authors.forename: Tijen
authors.initials: T
authors.lastname: Önkol
authors.forename: Adnan
authors.initials: A
authors.lastname: Menevşe
authors.forename: Kevser
authors.initials: K
authors.lastname: Erol
authors.forename: M Fethi
authors.initials: MF
authors.lastname: Sahin
mesh_terms: D000818:Animals; D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000494:pharmacology; D049109:Cell Proliferation / Q000187:drug effects; D002470:Cell Survival / Q000187:drug effects; D004305:Dose-Response Relationship, Drug; D015195:Drug Design; D004354:Drug Screening Assays, Antitumor; D004967:Estrogens / Q000378:metabolism*; D005260:Female; D006801:Humans; D015394:Molecular Structure; D051381:Rats; D017207:Rats, Sprague-Dawley; D011960:Receptors, Estrogen / Q000037:antagonists & inhibitors / Q000378:metabolism; D012457:Salicylamides / Q000737:chemistry* / Q000494:pharmacology*; D020156:Salicylic Acid / Q000737:chemistry* / Q000494:pharmacology*; D013329:Structure-Activity Relationship; D014407:Tumor Cells, Cultured; D014599:Uterus / Q000187:drug effects* / Q000473:pathology
chemical_list: D000970:Antineoplastic Agents; D004967:Estrogens; D011960:Receptors, Estrogen; D012457:Salicylamides; C031060:salicylamide; D020156:Salicylic Acid