Structure-Activity Relationships and Potent Cytotoxic Activities of Terphenyllin Derivatives from a Small Compound Library
Structure-Activity Relationships and Potent Cytotoxic Activities of Terphenyllin Derivatives from a Small Compound Library
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小型化合物库中三联苯衍生物的结构-活性关系和有效的细胞毒活性
DOI：
10.1002/cbdv.202000207
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发表时间：
2020-06-17
影响因子：
2.9
通讯作者：
Shao, Chang-Lun
中科院分区：
文献类型：
--
作者：
Haider, Waqas;Xu, Wei-Feng;Shao, Chang-Lun
建立了一个120个化合物的小型文库，其中包括70个新的天然产物三苯基的烷基化衍生物，以及以前报道的45个衍生物和4个天然对三苯基类似物。这70个新的衍生物是半合成的，并对四种癌细胞株的细胞毒活性进行了评估。有趣的是，2‘，4’-二乙氧基三苯基、2‘，4，4’-三异丙氧基三苯基、2‘，4’-二(环戊氧基)三苯基和2‘，4’-双(环戊氧基)三苯基具有较强的活性，其IC(50)值在0.13~5.51亩M之间，与阳性对照阿霉素相似。初步的构效关系表明，乙基、烯丙基、炔丙基、异丙基、溴丙基、异戊烯基、环丙基甲基和环戊基甲基等烷基取代基的引入对提高细胞毒性具有重要意义。
A small library of 120 compounds was established with seventy new alkylated derivatives of the natural product terphenyllin, together with 45 previous reported derivatives and four naturalp-terphenyl analogs. The 70 new derivatives were semi-synthesized and evaluated for cytotoxic activities against four cancer cell lines. Interestingly, 2 ',4 ''-diethoxyterphenyllin, 2 ',4,4 ''-triisopropoxyterphenyllin, and 2 ',4 ''-bis(cyclopentyloxy)terphenyllin showed potent activities with IC(50)values in a range from 0.13 to 5.51 mu M, which were similar to those of the positive control, adriamycin. The preliminary structure-activity relationships indicated that the introduction of alkyl substituents including ethyl, allyl, propargyl, isopropyl, bromopropyl, isopentenyl, cyclopropylmethyl, and cyclopentylmethyl are important for improving the cytotoxicity.