On the relationship of OSW-1 to the cephalostatins

Authors
Guo, CX LaCour, TG Fuchs, PL
Citation
Cx. Guo et al., On the relationship of OSW-1 to the cephalostatins, BIOORG MED, 9(3), 1999, pp. 419-424
Citations number
15
Categorie Soggetti
Chemistry & Analysis
Journal title
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
ISSN journal
0960894X → ACNP
Volume
9
Issue
3
Year of publication
1999
Pages
419 - 424
Database
ISI
SICI code
0960-894X(19990208)9:3<419:OTROOT>2.0.ZU;2-D
Abstract
Antineoplastic bis-steroidal (cephalostatin-type) analogues of the saponin OSW-1 were produced from a dihydroaglycone of OSW-1. The key aglycone 6H wa s obtained from 5 alpha-androstan-3 beta-ol-17-one in 8 steps (38% yield). The SAR of the aglycones, intermediates, and hybrid analogues provide insig hts regarding the proposed common role of C22-oxocarbenium ions in the bioa ctivity of both OSW-1 and cephalostatins (C) 1999 Elsevier Science Ltd. All rights reserved.