Cytotoxic 1,3-Thiazole and 1,2,4-Thiadiazole Alkaloids from Penicillium oxalicum: Structural Elucidation and Total Synthesis

草酸青霉菌中的细胞毒性 1,3-噻唑和 1,2,4-噻二唑生物碱:结构解析和全合成

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作者:Zheng Yang, Nianyu Huang, Bang Xu, Wenfeng Huang, Tianpeng Xie, Fan Cheng, Kun Zou

Abstract

Two new thiazole and thiadiazole alkaloids, penicilliumthiamine A and B (2 and 3), were isolated from the culture broth of Penicillium oxalicum, a fungus found in Acrida cinerea. Their structures were elucidated mainly by spectroscopic analysis, total synthesis and X-ray crystallographic analysis. Biological evaluations indicated that compound 1, 3a and 3 exhibit potent cytotoxicity against different cancer cell lines through inhibiting the phosphorylation of AKT/PKB (Ser 473), one of important cancer drugs target.

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