4.1 Article

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

Journal

RUSSIAN CHEMICAL BULLETIN
Volume 69, Issue 4, Pages 787-792

Publisher

SPRINGER
DOI: 10.1007/s11172-020-2834-3

Keywords

4H-pyrrolo[3; 2; 1-ij]quinoline-1; 2-dione; N-bromosuccinimide; piperazine; nucleophilic substitution; hybrid molecule; protein kinase

Funding

  1. Russian Science Foundation [18-74-10097]
  2. Russian Science Foundation [18-74-10097] Funding Source: Russian Science Foundation

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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 mu mol L-1 were obtained.

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