Synthesis of 4H-pyrrolo[3,2,1-ij]quinoline-1,2-diones containing a piperazine fragment and study of their inhibitory properties against protein kinases

被引:0
作者
N. P. Novichikhina
A. S. Shestakov
A. Yu. Potapov
E. A. Kosheleva
G. V. Shatalov
V. N. Verezhnikov
D. Yu. Vandyshev
I. V. Ledeneva
Kh. S. Shikhaliev
机构
[1] Voronezh State University,
来源
Russian Chemical Bulletin | 2020年 / 69卷
关键词
4; -pyrrolo[3,2,1-; ]quinoline-1,2-dione; -bromosuccinimide; piperazine; nucleophilic substitution; hybrid molecule; protein kinase;
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摘要
Hybrid compounds based on 4,4,6-trimethyl-4H-pyrrolo[3,2,1-ij]quinoline-1,2-diones containing a piperazine fragment were synthesized. Their inhibitory activity against protein kinases NPM1-ALK, ALK, EGFR[L858R][T790], EGFR[L858R], JAK2, and JAK3 was investigated. Compounds with inhibitory activity against protein kinase JAK3 at a level of 16.7 µmol L−1 were obtained.
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页码:787 / 792
页数:5
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