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Bradbury RH Hales NJ Rabow AA Walker GE Acton DG Andrews DM Ballard P Brooks NA Colclough N Girdwood A Hancox UJ Jones O Jude D Loddick SA Mortlock AA 《Bioorganic & medicinal chemistry letters》2011,21(18):5442-5445
Chemical starting points were investigated for downregulation of the androgen receptor as an approach to treatment of advanced prostate cancer. Although prototypic steroidal downregulators such as 6a designed for intramuscular administration showed insufficient cellular potency, a medicinal chemistry program derived from a novel androgen receptor ligand 8a led to 6-[4-(4-cyanobenzyl)piperazin-1-yl]-3-(trifluoromethyl)[1,2,4]triazolo[4,3-b]pyridazine (10b), for which high plasma levels following oral administration in a preclinical model compensate for moderate cellular potency. 相似文献
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