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Synthesis of spiro-tetrahydrothiopyran-oxindoles by Michael–aldol cascade reactions: discovery of potential P53-MDM2 inhibitors with good antitumor activity

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Abstract

Using proline as the catalyst, an organocatalytic Michael–aldol cascade reaction was developed for the synthesis of spiro-tetrahydrothiopyran oxindoles. The highly functionalized scaffold was assembled in moderate to good yields (51–78%) and excellent diastereoselectivities (>20 : 1 dr). Interestingly, the oxindoles displayed moderate to good in vitro antitumor activities and were validated as p53-MDM2 inhibitors, which represented promising lead compounds for antitumor drug discovery.

Graphical abstract: Synthesis of spiro-tetrahydrothiopyran-oxindoles by Michael–aldol cascade reactions: discovery of potential P53-MDM2 inhibitors with good antitumor activity

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Publication details

The article was received on 07 Nov 2017, accepted on 21 Dec 2017 and first published on 21 Dec 2017


Article type: Paper
DOI: 10.1039/C7OB02726E
Citation: Org. Biomol. Chem., 2018, Advance Article
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    Synthesis of spiro-tetrahydrothiopyran-oxindoles by Michael–aldol cascade reactions: discovery of potential P53-MDM2 inhibitors with good antitumor activity

    S. Wang, S. Chen, Z. Guo, S. He, F. Zhang, X. Liu, W. Chen, S. Zhang and C. Sheng, Org. Biomol. Chem., 2018, Advance Article , DOI: 10.1039/C7OB02726E

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