Functionalized Spiroindolines with Anticancer Activity through a Metal-Free Post-Ugi Diastereoselective One-Pot Cascade Reaction

Zhi Gang Xu, Shi Qiang Li, Jiang Ping Meng, Dian Yong Tang, Liu Jun He, Jie Lei, Hui Kuan Lin, Hong Yu Li, Zhong Zhu Chen

Research output: Contribution to journalArticle

4 Scopus citations

Abstract

A post-Ugi diastereoselective one-pot cascade reaction requiring no metal catalyst was developed. The reaction scope was wide with mild conditions and good yields. A collection of spiroindolines was prepared by the protocol and screening tests in several difficult-to-inhibit cancer cell lines were conducted. The relationship of structure and anticancer activities was promising and in the Huh7 cell lines compound 16 j is more potent than Vinbalstine. The cyclization design strategy could be applicable to other multicomponent reactions (MCRs) for synthesizing bioactive and drug-like heterocycles.

Original languageEnglish (US)
Pages (from-to)6732-6736
Number of pages5
JournalChemistry - A European Journal
Volume24
Issue number26
DOIs
StatePublished - May 7 2018

Keywords

  • Ugi reaction
  • cyclization reactions
  • multicomponent reactions
  • spiroindolines
  • synthetic methods

ASJC Scopus subject areas

  • Catalysis
  • Chemistry(all)
  • Organic Chemistry

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