Design and synthesis of novel 1,2,3-triazole-pyrimidine-urea hybrids as potential anticancer agents

  • Bioorg Med Chem Lett. 2015 Mar 1;25(5):1124-8. doi: 10.1016/j.bmcl.2014.12.087.
Li-Ying Ma  1 ,  Bo Wang  1 ,  Lu-Ping Pang  1 ,  Miao Zhang  1 ,  Sai-Qi Wang  1 ,  Yi-Chao Zheng  1 ,  Kun-Peng Shao  1 ,  Deng-Qi Xue  1 ,  Hong-Min Liu  2
Affiliations
  • 1. New Drug Research & Development Center, School of Pharmaceutical Sciences, Zhengzhou University, No. 100, Avenue Kexue, Zhengzhou 450001, PR China.
  • 2. New Drug Research & Development Center, School of Pharmaceutical Sciences, Zhengzhou University, No. 100, Avenue Kexue, Zhengzhou 450001, PR China. Electronic address: [email protected].
PMID: 25655718 DOI: 10.1016/j.bmcl.2014.12.087
Abstract

A series of novel 1,2,3-triazole-pyrimidine-urea hybrids were designed, synthesized and evaluated for Anticancer activity against four selected Cancer cell lines (MGC-803, EC-109, MCF-7 and B16-F10). Majority of the synthesized compounds exhibited moderate to potent activity against all the Cancer cell lines assayed. Particularly, compounds 26, 30 and 38 exhibited excellent growth inhibition against B16-F10 with IC50 values of 32nM, 35nM and 42nM, respectively. Flow cytometry analysis demonstrated that compound 26 induced the cellular Apoptosis in a concentration-dependent manner.

Keywords
Anticancer; Apoptosis; Pyrimidine; Triazole; Urea.