Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
1376516 | Bioorganic & Medicinal Chemistry Letters | 2006 | 4 Pages |
Abstract
Two potential bioisosteres of the nonsteroidal antiandrogen bicalutamide, an imidazolidinone and an indole, were synthesized and tested for their androgen receptor binding. Indole was discovered to be a suitable bioisostere for the acyl anilide moiety in the parent compound. Several analogs in the indole series were found to be 10-fold better than bicalutamide in binding to the recombinant androgen receptor binding domain.
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Physical Sciences and Engineering
Chemistry
Organic Chemistry
Authors
James C. Lanter, James J. Fiordeliso, George F. Allan, Amy Musto, Do Won Hahn, Zhihua Sui,