Synthesis and biological evaluation of 2-amino-1-thiazolyl imidazoles as orally active anticancer agents

Wen Tai Li, Der Ren Hwang, Jen Shin Song, Ching Ping Chen, Tung Wei Chen, Chi Hung Lin, Jiunn Jye Chuu, Tzu Wen Lien, Tsu An Hsu, Chen Lung Huang, Huan Yi Tseng, Chu Chung Lin, Heng Liang Lin, Chung Ming Chang, Yu Sheng Chao, Chiung Tong Chen*

*Corresponding author for this work

Research output: Contribution to journalArticlepeer-review

10 Scopus citations


Designed from a high throughput screened hit compound, novel 2-amino-1-thiazolyl imidazoles were synthesized and demonstrated cytotoxicity against human cancer cells. 1-(4-Phenylthiazol-2-yl)-4-(thiophen-2-yl)- 1Himidazol- 2-amine (compound 2), a 2-amino-1-thiazolyl imidazole, inhibited tubulin polymerization, interacted with the colchicine-binding sites of tubulins, and caused cell cycle arrest at the G 2/M phase in human gastric cancer cells. Disruption of the microtubule structure in cancer cells by compound 2 was also observed. Compound 2 concentration-dependently inhibited the proliferation of cancer cells in histocultured human gastric and colorectal tumors. Given orally, compound 2 prolonged the lifespans of leukemia mice intraperitoneally inoculated with the murine P388 leukemic cells. We report 2-amino-1-thiazolyl imidazoles as a novel class of orally active microtubuledestabilizing anticancer agents.

Original languageEnglish
Pages (from-to)164-175
Number of pages12
JournalInvestigational New Drugs
Issue number1
StatePublished - Feb 2012


  • Apoptosis
  • Cell cycle arrest
  • Cytotoxicity
  • Leukemia
  • Microtubule
  • Orally active cancer therapeutics

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