HIV-inhibitory natural products .30. Structure-activity modifications of the HIV-1 inhibitors (+)-calanolide A and (-)-calanolide B

被引：88

作者：

Galinis, DL ^{[1
]}

Fuller, RW ^{[1
]}

McKee, TC ^{[1
]}

Cardellina, JH ^{[1
]}

Gulakowski, RJ ^{[1
]}

McMahon, JB ^{[1
]}

Boyd, MR ^{[1
]}

机构：

[1] NCI,LAB DRUG DISCOVERY RES & DEV,DEV THERAPEUT PROGRAM,DIV CANC TREATMENT DIAG & CTR,FREDERICK,MD 21702

来源：

JOURNAL OF MEDICINAL CHEMISTRY | 1996年 / 39卷 / 22期

关键词：

D O I：

10.1021/jm9602827

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

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.

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页码：4507 / 4510

页数：4

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