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Chemical Research in Chinese Universities

, Volume 32, Issue 6, pp 929–937 | Cite as

Synthesis, antitumor activity and preliminary structure-activity relationship of 2-aminothiazole derivatives

  • Hongshuang Li
  • Xinran Wang
  • Guiyun Duan
  • Chengcai Xia
  • Yuliang Xiao
  • Furong Li
  • Yanqing Ge
  • Guirong You
  • Junfen Han
  • Xiaopan Fu
  • Shanhui Tan
  • Rongwei Wang
Article
  • 92 Downloads

Abstract

In this paper, we described the synthesis of 2-aminothiazole sublibrary containing methyl, bromo, phenyl or butylidene at 4- or/and 5-position of its core. All target compounds were evaluated for their antitumor activities against human lung cancer cell line H1299 and human glioma cell line SHG-44. Among the compounds screened, 4,5,6,7-tetrahydrobenzo[d]thiazole(26b) exhibited the most potent antitumor activities with IC50 values of 4.89 and 4.03 μmol/L against the two tested cell lines, respectively. Preliminary structure-activity relationship(SAR) studies of these compound were subsequently investigated.

Keywords

2-Aminothiazole Antitumor activity Structure-activity relationship 

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Supplementary material

40242_2016_6304_MOESM1_ESM.pdf (2.2 mb)
Synthesis and evaluation of new DPA analogues as inhibitors of glycosyltransferases

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Copyright information

© Jilin University, The Editorial Department of Chemical Research in Chinese Universities and Springer-Verlag GmbH 2016

Authors and Affiliations

  • Hongshuang Li
    • 1
  • Xinran Wang
    • 1
  • Guiyun Duan
    • 1
  • Chengcai Xia
    • 1
  • Yuliang Xiao
    • 1
  • Furong Li
    • 1
  • Yanqing Ge
    • 1
  • Guirong You
    • 1
  • Junfen Han
    • 1
  • Xiaopan Fu
    • 1
  • Shanhui Tan
    • 1
  • Rongwei Wang
    • 1
  1. 1.School of Pharmaceutical SciencesTaishan Medical UniversityTaianP. R. China

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