Article
20-Aminosteroids as a novel class of selective and complete androgen receptor antagonists and inhibitors of prostate cancer cell growth.
Bioorganic & medicinal chemistry - 1 Oct 2010
Fousteris Manolis A, Schubert Undine, Roell Daniela, Roediger Julia, Bailis Nikolaos, Nikolaropoulos Sotiris S, Baniahmad Aria, Giannis Athanassios
Abstract excerpt
Here, the synthesis and the evaluation of novel 20-aminosteroids on androgen receptor (AR) activity is reported. Compounds 11 and 18 of the series inhibit both the wild type and the T877A mutant AR-mediated transactivation indicating AR antagonistic function. Interestingly, minor structural changes such as stereoisomers of the amino lactame moiety exhibit preferences for antagonism among wild type and mutant AR....
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