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Biosynthesis of a Flavonol from a Flavanone by Establishing a One-pot Bienzymatic Cascade
Published on: August 14, 2019
Functionalized Spiroindolines with Anticancer Activity through a Metal-Free Post-Ugi Diastereoselective One-Pot
Zhi-Gang Xu1, Shi-Qiang Li1, Jiang-Ping Meng1
1Chongqing Engineering Laboratory of, Targeted and Innovative Therapeutics, Chongqing Key Laboratory of Kinase Modulators as, Innovative Medicine, IATTI, Chongqing University of Arts and Sciences, No. 319 Honghe Ave., Yongchuan, Chongqing, 402160, P.R. China.
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.
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