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抗肿瘤剂。134. 作为细胞毒性、抗病毒剂及蛋白激酶C抑制剂的新型与链格孢菌素A和卡尔佛斯汀C相关的苝衍生物。

Antitumor agents. 134. New shiraiachrome-A- and calphostin-C-related perylene derivatives as cytotoxic and antiviral agents and inhibitors of protein kinase C.

作者信息

Wang H K, Xie J X, Chang J J, Hwang K M, Liu S Y, Ballas L M, Jiang J B, Lee K H

机构信息

Natural Products Laboratory, School of Pharmacy, University of North Carolina, Chapel Hill 27599.

出版信息

J Med Chem. 1992 Jul 24;35(15):2717-21. doi: 10.1021/jm00093a001.

DOI:10.1021/jm00093a001
PMID:1379638
Abstract

Shiraiachrome-A and -B have been isolated from the mycelium of the Chinese bamboo fungus Shiraia bambusicola as the cytotoxic principles. A series of new perylene derivatives (7-27) related to Shiraiachrome-A and -B as well as Calphostin-C have been synthesized and evaluated for their cytotoxicity, antiviral activity, and inhibitory activity against protein kinase C. The results indicated that 11 and 12 are potent cytotoxic agents against HCT-8, RPMI-7951, and TE-671 solid tumor cells, whereas 24 and 26 demonstrated strong antiviral activity against HSV-1 and HSV-2. Compound 10 is an inhibitor of protein kinase C.

摘要

从中国竹黄菌(Shiraia bambusicola)的菌丝体中分离出了竹红菌素-A和竹红菌素-B作为细胞毒性成分。合成了一系列与竹红菌素-A和竹红菌素-B以及卡尔佛司汀-C相关的新型苝衍生物(7 - 27),并对其细胞毒性、抗病毒活性和对蛋白激酶C的抑制活性进行了评估。结果表明,11和12对HCT - 8、RPMI - 7951和TE - 671实体瘤细胞具有强大的细胞毒性作用,而24和26对单纯疱疹病毒-1(HSV - 1)和单纯疱疹病毒-2(HSV - 2)表现出强大的抗病毒活性。化合物10是蛋白激酶C的抑制剂。

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