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.