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On the relationship of OSW-1 to the cephalostatins
1Department of Chemistry, Purdue University, West Lafayette, IN 47907, USA.
Bioorganic & Medicinal Chemistry Letters
|March 26, 1999
Abstract:
Antineoplastic bis-steroidal (cephalostatin-type) analogues of the saponin OSW-1 were produced from a dihydroaglycone of OSW-1. The key aglycone 6H was obtained from 5alpha-androstan-3beta-ol-17-one in 8 steps (38% yield). The SAR of the aglycones, intermediates, and hybrid analogues provide insights regarding the proposed common role of C22-oxocarbenium ions in the bioactivity of both OSW-1 and cephalostatins.