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Structure‐Activity Relationships and Potent Cytotoxic Activities of Terphenyllin Derivatives from a Small Compound Library
Chemistry & Biodiversity ( IF 2.9 ) Pub Date : 2020-06-17 , DOI: 10.1002/cbdv.202000207
Waqas Haider 1, 2 , Wei-Feng Xu 1, 2 , Min Liu 3 , Yan-Wei Wu 1, 2 , Yan-Fei Tang 1, 2 , Mei-Yan Wei 1, 4 , Chang-Yun Wang 1, 2 , Ling Lu 1, 2 , Chang-Lun Shao 1, 2
Affiliation  

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 natural p‐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 IC50 values in a range from 0.13 to 5.51 μM, 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.

中文翻译:

来自小型化合物库的三联苯林衍生物的构效关系和有效的细胞毒活性

建立了一个包含 120 种化合物的小型库,其中包含 70 种新的天然产物三联苯的烷基化衍生物,以及 45 种先前报道的衍生物和四种天然对三联苯类似物。对 70 种新衍生物进行了半合成,并评估了对四种癌细胞系的细胞毒性活性。有趣的是,2',4''-二乙氧基三联苯林、2',4,4''-三异丙氧基三联苯林和2',4''-双(环戊氧基)三联苯林显示出有效的活性,IC50 值范围为0.13 至5.51 μM,与阳性对照阿霉素相似。初步的构效关系表明,引入包括乙基、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在内的烷基取代基对于提高细胞毒性很重要。
更新日期:2020-06-17
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