New Cytotoxic 1,2,4-Thiadiazole Alkaloids from the Ascidian Polycarpa aurata

被引：38

作者：

Cong-Dat Pham ^{[1
]}

Weber, Horst ^{[2
]}

Hartmann, Rudolf ^{[3
]}

Wray, Victor ^{[4
]}

Lin, Wenhan ^{[5
]}

Lai, Daowan ^{[1
]}

Proksch, Peter ^{[1
]}

机构：

[1] Univ Dusseldorf, Inst Pharmaceut Biol & Biotechnol, D-40225 Dusseldorf, Germany

[2] Univ Dusseldorf, Inst Pharmaceut & Med Chem, D-40225 Dusseldorf, Germany

[3] Forschungszentrum Julich, Inst Complex Syst ICS 6, D-52425 Julich, Germany

[4] Helmholtz Ctr Infect Res, D-38124 Braunschweig, Germany

[5] Peking Univ, State Key Lab Nat & Biomimet Drugs, Beijing 100191, Peoples R China

来源：

ORGANIC LETTERS | 2013年 / 15卷 / 09期

关键词：

DERIVATIVES;

D O I：

10.1021/ol400791n

中图分类号：

O62 [有机化学];

学科分类号：

070303 ; 081704 ;

摘要：

Two new alkaloids, polycarpathiamines A and B (1 and 2), were isolated from the ascidian Polycarpa aurata. Their structures were unambiguously determined by 1D, 2D NMR, and HRESIMS measurements and further confirmed by comparison with a closely related analogue, 3-dimethylamino-5-benzoy1-1,2,4-thiadiazole (4), that was prepared by chemical synthesis. Compounds 1 and 2 both feature an uncommon 1,2,4-thiadiazole ring whose biosynthetic origin is proposed. Compound 1 showed significant cytotoxic activity against L5178Y murine lymphoma cells (IC50 0.41 mu M).

引用

页码：2230 / 2233

页数：4

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