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ID: ALA1144953

Journal: Bioorg Med Chem Lett

Title: Anti-androgens with full antagonistic activity toward human prostate tumor LNCaP cells with mutated androgen receptor.

Authors: Ishioka T, Tanatani A, Nagasawa K, Hashimoto Y.

Abstract: Anti-androgens were designed based on the principle of inhibiting the folding of helix 12 of the nuclear androgen receptor. The prepared anti-androgens exhibited full antagonistic activity toward human prostate tumor LNCaP cells with T877A point-mutated nuclear androgen receptor, as far as examined, towards which other known anti-androgens, including hydroxyflutamide, are inactive or act as androgen agonists.

CiteXplore: 12873487

DOI: 10.1016/s0960-894x(03)00575-4