2008

Fused pyridine derivativesR 0450 Discovery of a Novel Series of Nonsteroidal Androgen Receptor Modulators:

5- or 6-Oxachrysen-2-ones. — Design and synthesis of a novel series of oxychryse-none derivatives are described. Results of preliminary SAR studies show that com-pound (IVb) possesses more potent androgen receptor agonist activity than dihydrotes-tosterone, whereas compound (XIIb) is a potent antagonist similar to bicalutamide. — (ZHAO*, S.; SHEN, Y.; VAN OEVEREN, A.; MARSCHKE, K. B.; ZHI, L.; Bioorg. Med. Chem. Lett. 18 (2008) 11, 3431-3435; Discovery Res., Ligand Pharm., Inc., San Diego, CA 92121, USA; Eng.) — H. Toeppel

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