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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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