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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学科分类号：
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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