Zhou Chunmei, Wang Lin, Zhang Minglong, Zhao Zhizhong, Zhang Xingquan, Chen Xianghong , Chen Hongshan, . SYNTHESIS AND ANTI-HIV ACTIVITY OF (±)-CALANOLIDE A AND ITS ANALOGUESJ. Acta Pharmaceutica Sinica, 1999, 34(9): 673-678.
Citation: Zhou Chunmei, Wang Lin, Zhang Minglong, Zhao Zhizhong, Zhang Xingquan, Chen Xianghong , Chen Hongshan, . SYNTHESIS AND ANTI-HIV ACTIVITY OF (±)-CALANOLIDE A AND ITS ANALOGUESJ. Acta Pharmaceutica Sinica, 1999, 34(9): 673-678.
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SYNTHESIS AND ANTI-HIV ACTIVITY OF (±)-CALANOLIDE A AND ITS ANALOGUES

    Abstract
  • AIM: To study the synthesis of (±)-calanolide A(5) and its analogues 11-demethyl and 6,6,11-demethyl calanolide A. METHODS AND RESULTS: (±)-Calanolide A(5) was synthesized by a four-step approach starting from phloroglucinol, via Pechmann reaction, Friedel-Crafts acylation, chromenylation and Luche reduction. (±)-Calanolide A analogues were also synthesized by the same methods. CONCLUSION: Anti-HIV test showed that the synthesized (±)-calanolide A markedly inhibited the accumulation of HIV-P24 antigen in Human PBMC cell with an IC50 of 0.83 μm and the therapeutic index (TI, TC50/IC50) was 34. The antiviral test of the analogues are in progress.
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