Chemical Papers

, Volume 73, Issue 2, pp 355–364 | Cite as

Synthesis and biological evaluation of 2,4-disubstituted thiazole amide derivatives as anticancer agent

  • Zhi-Hua Zhang
  • Hong-Mei Wu
  • Sai-Nan Deng
  • Rui-Xia Chai
  • Muriira Cyrus Mwenda
  • Yuan-Yuan Peng
  • Dong CaiEmail author
  • Yu ChenEmail author
Original Paper


A series of novel 2,4-disubstituted thiazole amide derivatives were synthesized, and their antiproliferative activities were tested. Some of these compounds displayed good antiproliferative activity, especially for HT29 cell. Among these compounds, compound 5b inhibits A549, HeLa, HT29 and Karpas299 cells with IC50 values of 8.64, 6.05, 0.63 and 13.87 μM, respectively. The western blot analysis and docking study provide important clues for further optimization of compound 5b as a potential c-Met inhibitor.


Thiazole derivatives Synthesis Anticancer activity 



This work was supported by the National Natural Science Foundation of China (No. 21601075), the Natural Science Foundation of Liaoning Province (Nos. 2015020249, 20170540396) and General Research Projects of Liaoning Provincial Department of Education (No. JQL201715410).

Supplementary material

11696_2018_587_MOESM1_ESM.docx (1.4 mb)
Supplementary material 1 (DOCX 1473 kb)


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Copyright information

© Institute of Chemistry, Slovak Academy of Sciences 2018

Authors and Affiliations

  • Zhi-Hua Zhang
    • 1
  • Hong-Mei Wu
    • 1
  • Sai-Nan Deng
    • 2
  • Rui-Xia Chai
    • 2
  • Muriira Cyrus Mwenda
    • 2
  • Yuan-Yuan Peng
    • 2
  • Dong Cai
    • 3
    Email author
  • Yu Chen
    • 4
    Email author
  1. 1.School of Chemical and Environmental EngineeringLiaoning University of TechnologyJinzhouChina
  2. 2.College of PharmacyJinzhou Medical UniversityJinzhouChina
  3. 3.College of Basic ScienceJinzhou Medical UniversityJinzhouChina
  4. 4.School of Life Science and BiopharmaceuticsShenyang Pharmaceutical UniversityShenyangChina

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