Small-molecule androgen receptor downregulators as an approach to treatment of advanced prostate cancer.

Robert H Bradbury,Neil J Hales,Alfred A Rabow,Graeme E Walker,David G Acton,David M Andrews,Peter Ballard,Nigel A N Brooks,Nicola Colclough,Alan Girdwood,Urs J Hancox,Owen Jones,David Jude,Sarah A Loddick,Andrew A Mortlock

Bioorganic & Medicinal Chemistry Letters（2011）

引用 48|浏览37

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摘要

As an approach to treatment of advanced prostate cancer, a medicinal chemistry program derived from a novel androgen receptor ligand 8a led to androgen receptor downregulator (10b), for which high plasma levels following oral administration in a preclinical model compensate for moderate cellular potency.

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关键词

Prostate cancer,Androgen receptor downregulator,Androgen antagonist

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