title: Cytotoxic 1,3-Thiazole and 1,2,4-Thiadiazole Alkaloids from Penicillium oxalicum: Structural Elucidation and Total Synthesis.
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.
authors.affiliation: Hubei Key Laboratory of Natural Products Research and Development, College of Biological and Pharmaceutical Sciences, China Three Gorges University, Yichang 443002, China. yangzctgu@sina.com.
authors.forename: Zheng
authors.initials: Z
authors.lastname: Yang
authors.affiliation: Hubei Key Laboratory of Natural Products Research and Development, College of Biological and Pharmaceutical Sciences, China Three Gorges University, Yichang 443002, China. hny115@126.com.
authors.forename: Nianyu
authors.initials: N
authors.lastname: Huang
authors.affiliation: Hubei Key Laboratory of Natural Products Research and Development, College of Biological and Pharmaceutical Sciences, China Three Gorges University, Yichang 443002, China. xubang08@163.com.|China Three Gorges University People's Hospital &amp; Yichang First People's Hospital, Yichang 443000, China. xubang08@163.com.
authors.forename: Bang
authors.initials: B
authors.lastname: Xu
authors.affiliation: Hubei Key Laboratory of Natural Products Research and Development, Medical College, China Three Gorges University, Yichang 443002, China. xyyxy1999@aliyun.com.
authors.forename: Wenfeng
authors.initials: W
authors.lastname: Huang
authors.affiliation: Hubei Key Laboratory of Natural Products Research and Development, College of Biological and Pharmaceutical Sciences, China Three Gorges University, Yichang 443002, China. sxdxxtp@foxmail.com.
authors.forename: Tianpeng
authors.initials: T
authors.lastname: Xie
authors.affiliation: Hubei Key Laboratory of Natural Products Research and Development, College of Biological and Pharmaceutical Sciences, China Three Gorges University, Yichang 443002, China. fancy1351@163.com.
authors.forename: Fan
authors.initials: F
authors.lastname: Cheng
authors.affiliation: Hubei Key Laboratory of Natural Products Research and Development, College of Biological and Pharmaceutical Sciences, China Three Gorges University, Yichang 443002, China. kzou@ctgu.edu.cn.
authors.forename: Kun
authors.initials: K
authors.lastname: Zou
mesh_terms: D000470:Alkaloids / Q000138:chemical synthesis* / Q000302:isolation & purification / Q000494:pharmacology; D000818:Animals; D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000302:isolation & purification / Q000494:pharmacology; D045744:Cell Line, Tumor; D002470:Cell Survival / Q000187:drug effects; D018360:Crystallography, X-Ray; D003603:Cytotoxins / Q000138:chemical synthesis* / Q000302:isolation & purification / Q000494:pharmacology; D015870:Gene Expression; D006110:Grasshoppers / Q000382:microbiology; D006801:Humans; D015394:Molecular Structure; D010407:Penicillium / Q000737:chemistry* / Q000302:isolation & purification; D051057:Proto-Oncogene Proteins c-akt / Q000037:antagonists & inhibitors / Q000235:genetics / Q000378:metabolism; D013830:Thiadiazoles / Q000138:chemical synthesis* / Q000302:isolation & purification / Q000494:pharmacology; D013844:Thiazoles / Q000138:chemical synthesis* / Q000302:isolation & purification / Q000494:pharmacology
chemical_list: D000470:Alkaloids; D000970:Antineoplastic Agents; D003603:Cytotoxins; D013830:Thiadiazoles; D013844:Thiazoles; D051057:Proto-Oncogene Proteins c-akt
keywords: Penicillium oxalicum; alkaloids; cytotoxicity; structure elucidation; total synthesis