909-13-7Relevant academic research and scientific papers
Structure-activity modifications of the HIV-1 inhibitors (+)-calanolide A and (-)-calanolide B
Galinis, Deborah L.,Fuller, Richard W.,McKee, Tawnya C.,Cardellina II, John H.,Gulakowski, Robert J.,McMahon, James B.,Boyd, Michael R.
, p. 4507 - 4510 (2007/10/03)
The Δ7,8 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.
