期刊
JOURNAL OF MEDICINAL CHEMISTRY
卷 60, 期 9, 页码 4086-4092出版社
AMER CHEMICAL SOC
DOI: 10.1021/acs.jmedchem.7b00062
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资金
- Deutsche Forschungsgemeinschaft [FR 3002/1-1]
STS and 17 beta-HSD1 are attractive targets for the treatment of estrogen-dependent diseases like endometriosis and breast cancer. The simultaneous inhibition of both enzymes appears more promising than blockage of either protein alone. We describe a designed multiple ligand approach resulting in highly potent dual inhibitors. The most interesting compound 9 showed nanomolar IC50 values for both proteins, membrane permeability, and no interference with estrogen receptors. It efficiently reversed E1S- and E1-induced T47D cell proliferation.
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