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
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
收藏
页码:2230 / 2233
页数:4
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