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Abstract <p>Eight novel 2-[(substituted)acetamido]thiazole-4-carboxylates were designed and synthesized as potential anticancer agents. The synthesized compounds were tested for in vitro cytotoxic activity against Panc-1 cells by the MTT assay and showed significant inhibition of cell proliferation. At 90 μM, ethyl 2-[2-(dibutylamino)acetamido]- and 2-[2-(4-methylpiperidin-1-yl)acetamidothiazole-carboxylates inhibited proliferation by &gt; 50%, with the former demonstrating a particularly strong potency (IC<sub>50</sub> = 43.08 μM<b>)</b>. Further experiments showed the ethyl 2-(2-(dibutylamino)acetamido)thiazole-4-carboxylate also markedly inhibited Panc-1 cell migration, invasion, and adhesion, which positions this compound as a promising candidate for anticancer drug development.</p>

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Synthesis, Characterization, and Anticancer Activity of 2-Aminothiazole Derivatives

  • 期刊论文

  • 发表日期：

    2025年5月1日

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  • Shu-Tong Han,
  • Cong Qi,
  • Zhao-Yuan Zhang,
  • Wei Hong,
  • Ran He,
  • Peng-Hong Hu,
  • Yao-Yao Cao,
  • Yuan-Fen Zhai,
  • Da-Hua Shi

摘要

Abstract

Eight novel 2-[(substituted)acetamido]thiazole-4-carboxylates were designed and synthesized as potential anticancer agents. The synthesized compounds were tested for in vitro cytotoxic activity against Panc-1 cells by the MTT assay and showed significant inhibition of cell proliferation. At 90 μM, ethyl 2-[2-(dibutylamino)acetamido]- and 2-[2-(4-methylpiperidin-1-yl)acetamidothiazole-carboxylates inhibited proliferation by > 50%, with the former demonstrating a particularly strong potency (IC50 = 43.08 μM). Further experiments showed the ethyl 2-(2-(dibutylamino)acetamido)thiazole-4-carboxylate also markedly inhibited Panc-1 cell migration, invasion, and adhesion, which positions this compound as a promising candidate for anticancer drug development.