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  3. The synthesis and antileukemic activity of 5-substituted thiazolyl urea derivatives

The synthesis and antileukemic activity of 5-substituted thiazolyl urea derivatives

  • Bioorg Med Chem Lett. 2025 Jan 1:115:130018. doi: 10.1016/j.bmcl.2024.130018.
Cheng Peng 1,  Li Sheng 2,  Gao-Ya Xu 2,  Xiao-Lei Qi 1,  Yu-Bo Zhou 2,  Jia-Li 3,  Yong-Mei Cui 4
Affiliations

Affiliations

  • 1 Department of Chemistry, Innovative Drug Research Center, College of Sciences, Shanghai University, Shanghai 200444, China.
  • 2 State Key Laboratory of Drug Research, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Shanghai 201203, China.
  • 3 State Key Laboratory of Drug Research, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Shanghai 201203, China. Electronic address: jli@simm.ac.cn.
  • 4 Department of Chemistry, Innovative Drug Research Center, College of Sciences, Shanghai University, Shanghai 200444, China. Electronic address: ymcui@shu.edu.cn.
PMID: 39536837 DOI: 10.1016/j.bmcl.2024.130018
Abstract

A series of novel 5-substituted thiazolyl urea derivatives were synthesized and evaluated for their efficacy as antileukemic agents against two human leukemic cell lines (THP-1 and MV-4-11). Results showed that the activities of the investigated compounds were quite sensitive to the positions and properties of the aromatic substituents. Among these compounds, compound 12k showed the highest activity with IC50 values of 29 ± 0.3 nM for THP-1 cells and 98 ± 10 nM for MV-4-11 cells.

Keywords

Antileukemic; SAR; Synthesis; Thiazolyl; Urea.

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