Functionalized Spiroindolines with Anticancer Activity through a Metal-Free Post-Ugi Diastereoselective One-Pot Cascade Reaction
| Autor: | Hong-yu Li, Jie Lei, Shi-Qiang Li, Zhi-Gang Xu, Liu Jun He, Hui Kuan Lin, Dian Yong Tang, Jiang Ping Meng, Zhong Zhu Chen |
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| Rok vydání: | 2018 |
| Předmět: |
Indoles
Screening test Cell Survival Molecular Conformation Antineoplastic Agents Stereoisomerism Crystallography X-Ray 010402 general chemistry 01 natural sciences Article Catalysis Cascade reaction Cell Line Tumor Humans Spiro Compounds Metal catalyst Cell survival 010405 organic chemistry Chemistry Organic Chemistry Huh7 cell General Chemistry Combinatorial chemistry 0104 chemical sciences Cyclization Metals Ugi reaction Cancer cell lines |
| Zdroj: | Chemistry - A European Journal. 24:6732-6736 |
| ISSN: | 0947-6539 |
| DOI: | 10.1002/chem.201801081 |
| Popis: | 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. |
| Databáze: | OpenAIRE |
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