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. Epub 2024 Nov 12.

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.

MeSH terms

  • Antineoplastic Agents* / chemical synthesis
  • Antineoplastic Agents* / chemistry
  • Antineoplastic Agents* / pharmacology
  • Cell Line, Tumor
  • Cell Proliferation / drug effects
  • Dose-Response Relationship, Drug
  • Drug Screening Assays, Antitumor*
  • Humans
  • Leukemia / drug therapy
  • Leukemia / pathology
  • Molecular Structure
  • Structure-Activity Relationship
  • Thiazoles* / chemical synthesis
  • Thiazoles* / chemistry
  • Thiazoles* / pharmacology
  • Urea* / analogs & derivatives
  • Urea* / chemical synthesis
  • Urea* / chemistry
  • Urea* / pharmacology

Substances

  • Urea
  • Antineoplastic Agents
  • Thiazoles