ANTI-AIDS AGENTS 31 - SYNTHESIS AND ANTI-HIV ACTIVITY OF 4-SUBSTITUTED 3',4'-DI-O-(-)-CAMPHANOYL-(-CIS-KHELLACTONE (DCK) THIOLACTONE ANALOGS())

Authors
YANG ZY XIA Y XIA P COSENTINO LM LEE KH
Citation
Zy. Yang et al., ANTI-AIDS AGENTS 31 - SYNTHESIS AND ANTI-HIV ACTIVITY OF 4-SUBSTITUTED 3',4'-DI-O-(-)-CAMPHANOYL-(-CIS-KHELLACTONE (DCK) THIOLACTONE ANALOGS()), Bioorganic & medicinal chemistry letters, 8(12), 1998, pp. 1483-1486
Citations number
7
Categorie Soggetti
Chemistry Inorganic & Nuclear","Chemistry Medicinal
Journal title
Bioorganic & medicinal chemistry letters → ACNP
ISSN journal
0960894X
Volume
8
Issue
12
Year of publication
1998
Pages
1483 - 1486
Database
ISI
SICI code
0960-894X(1998)8:12<1483:AA3-SA>2.0.ZU;2-2
Abstract
Four DCK-thiolactone analogs (3-6) were synthesized asymmetrically and evaluated for anti-HIV activity against HIV-1 replication in H9 lymph ocyte cells. Based on the functionality on the thiolactone-coumarin nu cleus, activity was in the order: methyl > H > propyl > benzyl. -3',4' -di-O-(-)-camphanoyl-(+)-cis-khelthiolactone (4) exhibited extremely p otent anti-HIV activity with EC50 and therapeutic index values of 0.00 718 mu M and > 21,300, respectively. (C) 1998 Elsevier Science Ltd. Al l rights reserved.