Synthesis and evaluation of hapalosin and analogs as MDR-reversing agents

Authors
O'Connell, CE Salvato, KA Meng, ZY Littlefield, BA Schwartz, CE
Citation
Ce. O'Connell et al., Synthesis and evaluation of hapalosin and analogs as MDR-reversing agents, BIOORG MED, 9(11), 1999, pp. 1541-1546
Citations number
27
Categorie Soggetti
Chemistry & Analysis
Journal title
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
ISSN journal
0960894X → ACNP
Volume
9
Issue
11
Year of publication
1999
Pages
1541 - 1546
Database
ISI
SICI code
0960-894X(19990607)9:11<1541:SAEOHA>2.0.ZU;2-L
Abstract
The marine natural product hapalosin and 22 analogs, which incorporated sys tematic substituent deletions or variations, were prepared. These compounds were evaluated in a cell-based assay for both MDR-reversing activity and g eneral cytotoxicity. Some substituent modifications resulted in lower cytot oxicities, but most structural changes were either detrimental to or did no t seriously alter the MDR-reversing activity. (C) 1999 Elsevier Science Ltd . All rights reserved.