Novel substituted aminothiazoles as potent and selective anti-hepatocellular carcinoma agents

Huagang Lu, John Rogowskyj, Wenquan Yu, Anu Venkatesh, Noshena Khan, Shigeki Nakagawa, Nicolas Goossens, Anna P. Koh, Takaaki Higashi, Ganesh Gunasekaran, Myron E. Schwarz, Spiros P. Hiotis, Xiaodong Xu, William Kinney, Yujin Hoshida, Timothy Block, Andrea Cuconati, Yanming Du

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6 Scopus citations


Based on our previous identification of a disubstituted aminothiazole termed HBF-0079 with promising selective toxicity for HCC-derived cell lines versus non-HCC liver lines, a series of tri-substituted aminothiazole derivatives were prepared and evaluated. This work resulted in the discovery of isopropyl 4-(pyrazin-2-yl)-2-(pyrimidin-2-ylamino)thiazole-5-carboxylate, 14, which displayed EC50value of 0.11 μM and more than 450 times of selectivity, and its methyl carbonate prodrug 24 with improved solubility in organic solvents. Furthermore, 14, was shown to reduce the proliferation of several liver cancer cells derived directly from patients.

Original languageEnglish
Pages (from-to)5819-5824
Number of pages6
JournalBioorganic and Medicinal Chemistry Letters
Issue number23
StatePublished - 2016


  • Hepatocellular carcinoma (HCC)
  • Prodrug
  • Substituted aminothiazole


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