ANTI-AIDS AGENTS .28. SYNTHESIS AND ANTI-HIV ACTIVITY OF METHOXY SUBSTITUTED 3',4'-DI-O-(-)-CAMPHANOYL-(-CIS-KHELLACTONE (DCK) ANALOGS())

Authors
TAKEUCHI Y XIE L COSENTINO LM LEE KH
Citation
Y. Takeuchi et al., ANTI-AIDS AGENTS .28. SYNTHESIS AND ANTI-HIV ACTIVITY OF METHOXY SUBSTITUTED 3',4'-DI-O-(-)-CAMPHANOYL-(-CIS-KHELLACTONE (DCK) ANALOGS()), Bioorganic & medicinal chemistry letters, 7(20), 1997, pp. 2573-2578
Citations number
7
Categorie Soggetti
Chemistry Inorganic & Nuclear","Chemistry Medicinal
Journal title
Bioorganic & medicinal chemistry letters → ACNP
ISSN journal
0960894X
Volume
7
Issue
20
Year of publication
1997
Pages
2573 - 2578
Database
ISI
SICI code
0960-894X(1997)7:20<2573:AA.SAA>2.0.ZU;2-H
Abstract
Four isomeric methoxy substituted DCK analogues (3-6) were asymmetrica lly synthesized from different starting materials. hoxy-3',4'-di-O-(-) -camphanoyl-(+)-cis-khellactone (5) exhibited extremely potent anti-HI V activity against HIV-1 replication in H9 lymphocyte cells with EC50 and therapeutic index values of 0.00038 mu M and >402,632, respectivel y, which are better than those of DCK and AZT in this assay. (C) 1997 Elsevier Science Ltd.