溶解循环
半合成
立体化学
IC50型
病毒复制
DNA复制
病毒
化学
生物
DNA
体外
病毒学
分子生物学
生物化学
作者
Yongsheng Lin,Qian Wang,Qiong Gu,Hongao Zhang,Jiang Cheng,Jia-Yuan Hu,Yan Wang,Yan Yuan,Jun Xu
标识
DOI:10.1021/acs.jnatprod.6b00415
摘要
(+)-Rutamarin inhibits EBV lytic DNA replication with an IC50 of 7.0 μM. (−)-Chalepin, a (−)-rutamarin derivative, was isolated from the whole plant of Ruta graveolens and used as a precursor of (−)-rutamarin. Altogether, 28 (−)-rutamarin derivatives were synthesized starting from (−)-chalepin. Of these, 16 compounds (2a–e, 3b–e, 3g, 4f, 4k, 4m–p) were found to be more potent against EBV lytic DNA replication than (−)-chalepin. Compounds 4m, 4n, and 4p exhibited IC50 values of 1.5, 0.32, and 0.83 μM and showed selectivity index values (SI) of 801, 211, and >120, respectively. Thus, compounds 4m, 4n, and 4p are considered promising leads for further laboratory investigation.
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