752225-71-1Relevant articles and documents
Stilbene-based inhibitors of estrone sulfatase with a dual mode of action in human breast cancer cells
Walter, Georg,Liebl, Renate,Von Angerer, Erwin
, p. 634 - 644 (2007/10/03)
Estrone sulfate (E1S) is an endogenous prodrug that delivers estrone and, subsequently, estradiol to target cells, after hydrolysis by the enzyme estrone sulfatase, which is active in various tissues including hormone-dependent breast cancer. Blockade of
Synthesis and biological evaluation of stilbene-based pure estrogen antagonists
Walter, Georg,Liebl, Renate,Von Angerer, Erwin
, p. 4659 - 4663 (2007/10/03)
The nonsteroidal estrogen diethylstilbestrol can be converted into potent antiestrogens devoid of agonist activity by introduction of side chains with appropriate functional groups. Replacement of one of the ethyl substituents in diethylstilbestrol by side chains with functional groups converted this potent estrogen into pure antiestrogens with the potential for the treatment of breast cancer. These agents completely suppressed estrogen receptor-mediated gene activation and inhibited the growth of estrogen-sensitive MCF-7 breast cancer cells in submicromolar concentrations. The most potent derivative displayed similar activity as fulvestrant (ICI 182,780) in vitro and in the mouse uterine weight test. Obviously, the stilbene structure can act as a substitute for estradiol in the development of pure estrogen antagonists.
