Cytotoxic Aaptamine Derivatives from the South China Sea Sponge Aaptos aaptos

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• 作者：Hao-Bing Yu ; Fan Yang ; Fan Sun ; Guo-Yi Ma ; Jian-Hong Gan ; Wen-Zhen Hu ; Bing-Nan Han ; Wei-Hua Jiao ; Hou-Wen Lin
• 刊名：Journal of Natural Products
• 出版年：2014
• 出版时间：September 26, 2014
• 年：2014
• 卷：77
• 期：9
• 页码：2124-2129
• 全文大小：270K
• ISSN：1520-6025

文摘

Nine new aaptamine derivatives (1鈥?b>9), together with three known related compounds (10鈥?b>12), have been isolated from the South China Sea sponge Aaptos aaptos. The structures of all compounds were unambiguously elucidated on the basis of spectroscopic analyses. Structurally, compound 1 possesses a piperidinyl group fused to a demethyl(oxy)aaptamine moiety, whereas compounds 3鈥?b>6 share an imidazole-fused 1H-benzo[de][1,6]naphthyridin-2(4H)-one skeleton. The cytotoxic activities of the compounds were evaluated against various human cancer cell lines, and compounds 2, 8, 11, and 12 showed potent cytotoxicities against HL60, K562, MCF-7, KB, HepG2, and HT-29 cells, with IC₅₀ values in the range of 0.03 to 8.5 渭M.