Skip to main page content
U.S. flag

An official website of the United States government

Dot gov

The .gov means it’s official.
Federal government websites often end in .gov or .mil. Before sharing sensitive information, make sure you’re on a federal government site.

Https

The site is secure.
The https:// ensures that you are connecting to the official website and that any information you provide is encrypted and transmitted securely.

Access keys NCBI Homepage MyNCBI Homepage Main Content Main Navigation
. 1996 Oct 25;39(22):4507-10.
doi: 10.1021/jm9602827.

Structure-activity modifications of the HIV-1 inhibitors (+)-calanolide A and (-)-calanolide B

D L Galinis  1 , R W Fuller, T C McKee, J H Cardellina 2nd, R J Gulakowski, J B McMahon, M R Boyd
Affiliations

Structure-activity modifications of the HIV-1 inhibitors (+)-calanolide A and (-)-calanolide B

D L Galinis et al. J Med Chem. .

Abstract

The delta 7,8 olefinic linkages within (+)-calanolide A(1) and (-)-calanolide B(2) were catalytically reduced to determine impact on the anti-HIV activity of the parent compounds. In addition, a series of structure modifications of the C-12 hydroxyl group in (-)-calanolide B was made to investigate the importance of that substituent to the HIV-1 inhibitory activity of these coumarins. A total of 14 analogs were isolated or prepared and compared to (+)-calanolide A and (-)-calanolide B in the NCI primary anti-HIV assay. While none of the compounds showed activity superior to the two unmodified leads, some structure-activity requirements were apparent from the relative anti-HIV potencies of the various analogs.

PubMed Disclaimer

LinkOut - more resources