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5-Alkylpyrrole-2-carboxaldehyde derivatives from the Chinese sponge Mycale lissochela and their PTP1B inhibitory activities

查看全文 作　　者：Duo-Qing [1]Xue;Hai-Li [1]Liu;Si-Han [1]Chen;Ernesto [2]Mollo;Margherita [2]Gavagnin;Jia [1]Li;Xu-Wen [1]Li;Yue-Wei [1]Guo 高影响力作者 机构地区：[1]State Key Laboratory of Drug Research, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Shanghai 201203, China;[2]Institute of Biomolecular Chemistry (ICB) of the National Research Council (CNR), Via Campi Flegrei 34, 80078, Pozzuoli, Napoli, Italy高影响力机构 出　　处：《Chinese Chemical Letters》索引2017年第28卷第6期,共4页高影响力期刊 基　　金：financially supported by the National Natural Science Foundation of China(Nos.41476063,81520108028,81273430,41306130 81302692,41676073,81603022);SCTSM Project from Shanghai Science and Technology Committee,Shanghai,China(Nos.14431901100,15431901000);The project from Institutes for Drug Discovery and Development,Chinese Academy of Sciences,China(No.CASIMM0120152039);the SKLDR/SIMM Projects from Shanghai Institute of MateriaMedica,China(No.SIMM 1501ZZ-03);support of 'Youth Innovation Promotion Association'(No.2016258) from Chinese Academy of Sciences;'Young Talent Supporting Project' from China Association for Science and Technology(No.2016QNRC001);Shanghai 'Pujiang Program'(No.16PJ1410600) 摘　　要：Two new 5-alkylpyrrole-2-carboxaldehyde derivatives,mycalenitrile-15(1) and mycalenitrile-16(2),along with five known related ones(3-7),were isolated from the South China Sea sponge Mycale lissochela.The structures of the new compounds were elucidated on the basis of extensive spectroscopic analysis and by comparison of their NMR data with those reported in the literature.In bioassay,compounds 1 and 7 exhibited significant PTPIB(Protein-tyrosine phosphatase 1B,a recognized target for diabetes and obesity) inhibitory activities with IC_(50) values of 8.6 and 3.1 μmoI/L,respectively.A preliminary SAR analysis of the isolated compounds with their PTP1 B inhibitory effects was described. 关 键 词：5-Alkylpyrrole-2-carboxaldehyde 海绵 Mycale lissochela PTP1B 禁止者 海洋的自然产品
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