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ID: ALA2331274

Journal: J Med Chem

Title: SAR based design of nicotinamides as a novel class of androgen receptor antagonists for prostate cancer.

Authors: Yang SH, Song CH, Van HT, Park E, Khadka DB, Gong EY, Lee K, Cho WJ.

Abstract: Molecular knowledge of pure antagonism and systematic SAR study offered a direction for structural optimization of DIMN to provide nicotinamides as a novel series of AR antagonists. Nicotinamides with extended linear scaffold bearing sterically bulky alkoxy groups on isoquinoline end were synthesized for H12 displacement. AR binding affinity and molecular basis of antiandrogenic effect establish the optimized derivatives, 7au and 7bb, as promising candidates of second generation AR antagonists for advanced prostate cancer.

CiteXplore: 23527816

DOI: 10.1021/jm3014103