1. Academic Validation
  2. Design, synthesis and antiproliferative activity studies of novel 1,2,3-triazole-dithiocarbamate-urea hybrids

Design, synthesis and antiproliferative activity studies of novel 1,2,3-triazole-dithiocarbamate-urea hybrids

  • Eur J Med Chem. 2013 Jun:64:99-110. doi: 10.1016/j.ejmech.2013.03.058.
Ying-Chao Duan 1 Yi-Chao Zheng Xiao-Chen Li Meng-Meng Wang Xian-Wei Ye Yuan-Yuan Guan Gai-Zhi Liu Jia-Xin Zheng Hong-Min Liu
Affiliations

Affiliation

  • 1 New Drug Research & Development Center, School of Pharmaceutical Sciences, Zhengzhou University, No. 100, Avenue Kexue, Zhengzhou 450001, PR China.
Abstract

A series of novel 1,2,3-triazole-dithiocarbamate-urea hybrids were designed, synthesized and their antiproliferative activities against four selected human Cancer cell lines were evaluated. The results showed that a number of the hybrids exhibited potent activity in selected human Cancer cell lines. Among them, compounds 27 and 34 showed broad spectrum Anticancer activity with IC50 values ranging from 1.62 to 20.84 μM and 0.76 to 13.55 μM, respectively. Interestingly, compounds 27 and 34, being very potent against MGC-803 cells, exhibited no significant cytotoxicity against normal human embryonic kidney cells at up to 55 μM and 70 μM, respectively. Evidences of cell cycle arrest and Apoptosis induction were obtained for the most effective compounds 27 and 34 by means of flow cytometry and microscopic techniques.

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