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中文摘要：
从海洋微生物发酵产物十字孢碱出发,合成12个新的PKC-412卤代衍生物1~12,其结构经1H NMR,13C NMR,IR和HRESIMS确定.用噻唑蓝(MTT)法测定了12个卤代衍生物对肿瘤细胞株HL-60,A549和Hela的细胞毒活性.结果表明,化合物4和10具有良好的细胞毒活性,对HL-60和A549两种肿瘤细胞株的IC50值在0.5~0.95μmol·L-1,与PKC-412活性相当,且苯甲酰胺片段的苯环上直接卤代提高了化合物对A549细胞的选择性,值得深入研究.
英文摘要：
Twelve new halogenated derivatives of PKC-412 were synthesized from the marine microbial natural product, staurosporine. Their structures were identified by 1H NMR, 13C NMR, IR and HRESIMS. The cytotoxicities of these halo-genated derivatives against HL-60, A549 and hela cell lines were evaluated using thiazolyl blue tetrazolium bromide (MTT) method. The results showed that compounds 4 and 10 displayed comparative cytotoxicity of PKC-412 against HL-60 and A549 cell lines with IC50 values of 0.5~0.95 μmol?L-1, and the halogenation on phenyl nucleus of benzamide moiety in-creased the selectivity of compounds to A549 cell, indicating a worth of further study.
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