A series of compounds containing a novel 3-carboxypiperidin-2-one scaffold based on the lead structure BMS-777607 were designed, synthesized and evaluated for their c-Met kinase inhibition and cytotoxicity against MKN45 cancer cell lines. The results indicated that five compounds exhibited significant inhibitory effect on c-Met with IC 50 values of 8.6−81 nM and four compounds showed potent inhibitory activity against MKN45 cell proliferation, with IC 50 s ranging from 0.57−16 μM.
The total synthesis of 2′,3′‐di‐O‐acetylfrangulin A (1) and prinoidin (2), which were isolated from Rhamnus nepalensis and showed significant cytotoxicity to KB cell line, was achieved for the first time. The structures of the two compounds were confirmed by 1H NMR, 13C NMR, 1H‐1H COSY, HMQC and HMBC.
The total synthesis of 2',3'-di-O-acetylfrangulin A (1) and prinoidin (2), which were isolated from Rhamnus nepalensis and showed significant cytotoxicity to KB cell line, was achieved for the first time. The structures of the two compounds were confirmed by 1 H NMR, 13 C NMR, 1 H-1 H COSY, HMQC and HMBC.
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