Synthesis of spiro-tetrahydrothiopyran-oxindoles by Michael–aldol cascade reactions: discovery of potential P53-MDM2 inhibitors with good antitumor activity†,10.1039/C7OB02726E

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Lactoyl-CoA 全氟丁基戊烷白叶藤碱全氟己基辛烷新白叶藤碱壳寡糖特色专题-生物多肽

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

Shengzheng Wang,Shuqiang Chen,Zhongjie Guo,Shipeng He,Fan Zhang,Xueying Liu,Weiping Chen,Shengyong Zhang,Chunquan Sheng

Organic & Biomolecular Chemistry Pub Date : 12/21/2017 00:00:00 , DOI:10.1039/C7OB02726E

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.