2. Academic Validation
  3. Syntheses and biological evaluation of 1,2,3-triazole and 1,3,4-oxadiazole derivatives of imatinib

Syntheses and biological evaluation of 1,2,3-triazole and 1,3,4-oxadiazole derivatives of imatinib

  • Bioorg Med Chem Lett. 2016 Mar 1;26(5):1419-27. doi: 10.1016/j.bmcl.2016.01.068.
Yong-Tao Li 1,  Jing-Han Wang 1,  Cheng-Wen Pan 1,  Fan-Fei Meng 1,  Xiao-Qian Chu 2,  Ya-hui Ding 3,  Wen-Zheng Qu 1,  Hui-ying Li 2,  Cheng Yang 1,  Quan Zhang 3,  Cui-Gai Bai 4,  Yue Chen 5
Affiliations

Affiliations

  • 1 The State Key Laboratory of Elemento-Organic Chemistry, College of Pharmacy, Collaborative Innovation Center of Chemical Science and Engineering (Tianjin), and Tianjin Key Laboratory of Molecular Drug Research, Nankai University, Tianjin 300071, PR China; High-throughput Molecular Drug Discovery Center, Tianjin International Joint Academy of BioMedicine, Tianjin 300457, PR China.
  • 2 High-throughput Molecular Drug Discovery Center, Tianjin International Joint Academy of BioMedicine, Tianjin 300457, PR China.
  • 3 The State Key Laboratory of Elemento-Organic Chemistry, College of Pharmacy, Collaborative Innovation Center of Chemical Science and Engineering (Tianjin), and Tianjin Key Laboratory of Molecular Drug Research, Nankai University, Tianjin 300071, PR China.
  • 4 High-throughput Molecular Drug Discovery Center, Tianjin International Joint Academy of BioMedicine, Tianjin 300457, PR China. Electronic address: baicuigai@tjab.org.
  • 5 The State Key Laboratory of Elemento-Organic Chemistry, College of Pharmacy, Collaborative Innovation Center of Chemical Science and Engineering (Tianjin), and Tianjin Key Laboratory of Molecular Drug Research, Nankai University, Tianjin 300071, PR China. Electronic address: yuechen@nankai.edu.cn.
PMID: 26850004 DOI: 10.1016/j.bmcl.2016.01.068
Abstract

Three novel series of 1,2,3-triazole and 1,3,4-oxadiazole derivatives of imatinib were prepared and evaluated in vitro for their cytostatic effects against a human chronic myeloid leukemia (K562), acute myeloid leukemia (HL60), and human leukemia stem-like cell line (KG1a). The structure-activity relationship was analyzed by determining the inhibitory rate of each imatinib analog. Benzene and piperazine rings were necessary groups in these compounds for maintaining inhibitory activities against the K562 and HL60 cell lines. Introducing a trifluoromethyl group significantly enhanced the potency of the compounds against these two cell lines. Surprisingly, some compounds showed significant inhibitory activities against KG1a cells without inhibiting common leukemia cell lines (K562 and HL60). These findings suggest that these compounds are able to inhibit leukemia stem-like cells.

Keywords

Chronic myelogenous leukemia; Imatinib; K562; KG-1a; Synthesis.

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