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

作　　者：Duo-Qing Xue Hai-Li Liu Si-Han Chen Ernesto Mollo Margherita Gavagnin Jia Li Xu-Wen Li Yue-Wei Guo 

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

出　　处：《Chinese Chemical Letters》2017年第6期1190-1193,共4页中国化学快报（英文版）

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.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 Sponge Mycale lissochela PTP1B inhibitor Marine natural product 

分 类 号：TQ460.1[化学工程—制药化工]