5-Alkylpyrrole-2-carboxaldehyde derivatives from the Chinese sponge Mycale lissochela and their PTP1B inhibitory activities |
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Authors: | Duo-Qing Xue Hai-Li Liu Si-Han Chen Ernesto Mollo Margherita Gavagnin Jia Li Xu-Wen Li Yue-Wei Guo |
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Institution: | a State Key Laboratory of Drug Research, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Shanghai 201203, China;
b Institute of Biomolecular Chemistry(ICB) of the National Research Council(CNR), Via Campi Flegrei 34, 80078, Pozzuoli, Napoli, Italy |
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Abstract: | 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 PTP1B (Protein-tyrosine phosphatase 1B, a recognized target for diabetes and obesity) inhibitory activities with IC50 values of 8.6 and 3.1 μmol/L, respectively. A preliminary SAR analysis of the isolated compounds with their PTP1B inhibitory effects was described. |
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Keywords: | 5-Alkylpyrrole-2-carboxaldehyde Sponge Mycale lissochela PTP1B inhibitor Marine natural product |
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