One-pot synthesis of natural-product inspired spiroindolines with anti-cancer activities

Shi Qiang Li, Wei Yan, Liu Jun He, Ming Zhang, Dian Yong Tang, Hong Yu Li, Zhong Zhu Chen, Zhi Gang Xu

Research output: Contribution to journalArticlepeer-review

5 Scopus citations


A post-Ugi/diastereoselective cascade reaction was developed to construct naturally existing spiroindolines via a facile and metal-free one-pot protocol. During the construction, a new C-C bond was formed through a selective 5-exo-dig indole cyclization on the propiolamide; and a new C-N bond was diastereoselectively formed which controlled the configuration of three chiral centers simultaneously. Screening data of several difficult-to-inhibit cancer cell lines demonstrated that (±)-6d could strongly inhibit colon cell U87 proliferation with an IC50 value of 0.19 ± 0.04 μM. Taken together, our research provided a novel and robust protocol towards the synthesis of spiroindolines and revealed their potential application as anti-cancer agents in diverse human cancer cell lines.

Original languageEnglish (US)
Pages (from-to)682-686
Number of pages5
JournalOrganic Chemistry Frontiers
Issue number3
StatePublished - Feb 7 2022
Externally publishedYes

ASJC Scopus subject areas

  • Organic Chemistry


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