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.
Keywords:
Penicillium oxalicum; alkaloids; cytotoxicity; structure elucidation; total synthesis.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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Alkaloids / chemical synthesis*
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Alkaloids / isolation & purification
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Alkaloids / pharmacology
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Animals
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Antineoplastic Agents / chemical synthesis*
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Antineoplastic Agents / isolation & purification
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Antineoplastic Agents / pharmacology
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Cell Line, Tumor
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Cell Survival / drug effects
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Crystallography, X-Ray
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Cytotoxins / chemical synthesis*
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Cytotoxins / isolation & purification
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Cytotoxins / pharmacology
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Gene Expression
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Grasshoppers / microbiology
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Humans
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Molecular Structure
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Penicillium / chemistry*
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Penicillium / isolation & purification
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Proto-Oncogene Proteins c-akt / antagonists & inhibitors
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Proto-Oncogene Proteins c-akt / genetics
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Proto-Oncogene Proteins c-akt / metabolism
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Thiadiazoles / chemical synthesis*
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Thiadiazoles / isolation & purification
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Thiadiazoles / pharmacology
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Thiazoles / chemical synthesis*
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Thiazoles / isolation & purification
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Thiazoles / pharmacology
Substances
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Alkaloids
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Antineoplastic Agents
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Cytotoxins
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Thiadiazoles
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Thiazoles
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Proto-Oncogene Proteins c-akt