Synthesis and evaluation of novel N-substituted N'-(3-hydroxy-17-oxoestra-1,3,5(10)-trien-2- and -4-yl)thiourea derivatives for binding to the estrogen receptor and cytotoxic activity on MCF-7 cells.
A novel series of estrone derivatives having a free 3-phenolic group with the 2- or 4-position substituted with a thiourea function was synthesized. None of the products showed significant binding to the estrogen receptor, and the cytotoxic activity on MCF-7 cells for VII and X was weak.
D000818:Animals; D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000378:metabolism / Q000494:pharmacology; D001943:Breast Neoplasms / Q000473:pathology; D002455:Cell Division / Q000187:drug effects; D002460:Cell Line; D055598:Chemical Phenomena; D002621:Chemistry; D004963:Estrenes / Q000138:chemical synthesis* / Q000378:metabolism / Q000494:pharmacology; D004965:Estrogen Antagonists / Q000138:chemical synthesis* / Q000378:metabolism / Q000494:pharmacology; D005260:Female; D006801:Humans; D066298:In Vitro Techniques; D051381:Rats; D011960:Receptors, Estrogen / Q000378:metabolism; D013890:Thiourea / Q000031:analogs & derivatives / Q000138:chemical synthesis / Q000378:metabolism / Q000494:pharmacology; D014599:Uterus / Q000378:metabolism
D000970:Antineoplastic Agents; D004963:Estrenes; D004965:Estrogen Antagonists; D011960:Receptors, Estrogen; D013890:Thiourea