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Issue 60, 2018
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Asymmetric synthesis of tetrahydroisoquinoline-fused spirooxindoles as Ras-GTP inhibitors that inhibit colon adenocarcinoma cell proliferation and invasion

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Abstract

Here we report the synthesis of a library of chiral THIQ-fused spirooxindoles, which combine two privileged scaffolds in antitumor medicinal chemistry. Some of the library members inhibit the proliferation and invasion ability of Ras-mutated colon adenocarcinoma cells. Mechanistic studies suggest that the most potent compound, 3m, inhibits Ras-GTP and thereby suppresses downstream signaling mediated by MAPK, PI3K-Akt and Wnt. Ultimately this leads to mitochondrial apoptosis.

Graphical abstract: Asymmetric synthesis of tetrahydroisoquinoline-fused spirooxindoles as Ras-GTP inhibitors that inhibit colon adenocarcinoma cell proliferation and invasion

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Publication details

The article was received on 13 Jun 2018, accepted on 04 Jul 2018 and first published on 11 Jul 2018


Article type: Communication
DOI: 10.1039/C8CC04732D
Citation: Chem. Commun., 2018,54, 8359-8362
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    Asymmetric synthesis of tetrahydroisoquinoline-fused spirooxindoles as Ras-GTP inhibitors that inhibit colon adenocarcinoma cell proliferation and invasion

    Q. Zhao, C. Peng, H. Huang, S. Liu, Y. Zhong, W. Huang, G. He and B. Han, Chem. Commun., 2018, 54, 8359
    DOI: 10.1039/C8CC04732D

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