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作者:

Hua, Liming (Hua, Liming.) | Cao, Tingting (Cao, Tingting.) | Lv, Yongjuan (Lv, Yongjuan.) | Ding, Yiming (Ding, Yiming.) | Yang, Leifu (Yang, Leifu.) | Zhang, Qiang (Zhang, Qiang.) | Guo, Mingzhou (Guo, Mingzhou.)

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Scopus SCIE PubMed

摘要:

A series of 4-((pyrazolo[1,5-a]pyrimidin-6-yl)-1H-pyrazol-1-yl)phenyl-3-benzamide derivatives and 4-((imidazo[1,2-b]pyridazin-3-yl)-1H-pyrazol-1-yl-)phenyl-3-benzamide derivatives were designed, synthesized as new BCR-ABL tyrosine kinase inhibitors by using combinational strategies of scaffold hopping and conformational constraint. These new compounds were screened for BCR-ABL1 kinase inhibitory activity, and most of them appeared good inhibitory activity against BCR-ABL1 kinase. One of the most potent compounds 16a strongly suppressed BCR-ABL1 kinase with IC50 value of 8.5 nM. The tested compounds 16a and 16i showed strong inhibitory activities against K562 with IC50 value of less than 2 nM. Molecular docking studies indicated that these compounds fitted well with the active site of BCR-ABL1 protein. The results showed these inhibitors may serve as lead compounds for further developing new drugs targeted BCR-ABL kinase. (C) 2016 Elsevier Ltd. All rights reserved.

关键词:

BCR-ABL inhibitors Bioactivity Chronic myeloid leukemia Molecular docking

作者机构:

  • [ 1 ] [Hua, Liming]Beijing Univ Technol, Coll Life Sci & Bioengn, Beijing 100124, Peoples R China
  • [ 2 ] [Cao, Tingting]Beijing Univ Technol, Coll Life Sci & Bioengn, Beijing 100124, Peoples R China
  • [ 3 ] [Lv, Yongjuan]Beijing Univ Technol, Coll Life Sci & Bioengn, Beijing 100124, Peoples R China
  • [ 4 ] [Ding, Yiming]Beijing Univ Technol, Coll Life Sci & Bioengn, Beijing 100124, Peoples R China
  • [ 5 ] [Yang, Leifu]Beijing Scitech MQ Pharmaceut Ltd, Beijing 101320, Peoples R China
  • [ 6 ] [Zhang, Qiang]Beijing Scitech MQ Pharmaceut Ltd, Beijing 101320, Peoples R China
  • [ 7 ] [Guo, Mingzhou]Chinese Peoples Liberat Army Gen Hosp, Beijing 100853, Peoples R China

通讯作者信息:

  • [Hua, Liming]Beijing Univ Technol, Coll Life Sci & Bioengn, Beijing 100124, Peoples R China

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来源 :

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

ISSN: 0960-894X

年份: 2016

期: 23

卷: 26

页码: 5830-5835

2 . 7 0 0

JCR@2022

ESI学科: CHEMISTRY;

ESI高被引阀值:147

中科院分区:3

被引次数:

WoS核心集被引频次: 8

SCOPUS被引频次: 9

ESI高被引论文在榜: 0 展开所有

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