RESOLUTION AND COMPARATIVE ANTI-HIV EVALUATION OF THE ENANTIOMERS OF CALANOLIDE-A AND CALANOLIDE-B

被引:54
作者
CARDELLINA, JH [1 ]
BOKESCH, HR [1 ]
MCKEE, TC [1 ]
BOYD, MR [1 ]
机构
[1] NCI,DIV CANC TREATMENT,DRUG DISCOVERY RES & DEV LAB,DEV THERAPEUT PROGRAM,FREDERICK,MD 21702
关键词
D O I
10.1016/0960-894X(95)00158-P
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
Methods for the chiral resolution of (+)-calanolide A and (-)-calanolide A from synthetic (+/-)-calanolide A, and of (+)-calanolide B and (-)-calanolide B (costatolide) from a scalemic mixture isolated from C. lanigerium, have been developed. Calanolide A was originally isolated as the pure (+) enantiomer from C. lanigerum, but now is also shown to occur as a scalemic mixture in latex of C. teysmannii. Interestingly, (+)-calanolide A and (-)-calanolide B are potent HIV-1 inhibitors, while (-)-calanolide A and (+)-calanolide B are inactive against the virus.
引用
收藏
页码:1011 / 1014
页数:4
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