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

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• 作者：Cong-Dat Pham ; Horst Weber ; Rudolf Hartmann ; Victor Wray ; Wenhan Lin ; Daowan Lai ; Peter Proksch
• 刊名：Organic Letters
• 出版年：2013
• 出版时间：May 3, 2013
• 年：2013
• 卷：15
• 期：9
• 页码：2230-2233
• 全文大小：235K
• 年卷期：v.15,no.9(May 3, 2013)
• ISSN：1523-7052

文摘

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-benzoyl-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 渭M).