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

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.

SUBMITTER: Xu ZG

PROVIDER: S-EPMC6042644 | biostudies-literature | 2018 May

REPOSITORIES: biostudies-literature

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

Xu Zhi-Gang ZG Li Shi-Qiang SQ Meng Jiang-Ping JP Tang Dian-Yong DY He Liu-Jun LJ Lei Jie J Lin Hui-Kuan HK Li Hong-Yu HY Chen Zhong-Zhu ZZ

Chemistry (Weinheim an der Bergstrasse, Germany) 20180420 26

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 appli ...[more]

PMID: 29676029

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