2. Academic Validation
  3. Design, synthesis and antiproliferative activity studies of novel dithiocarbamate-chalcone derivates

Design, synthesis and antiproliferative activity studies of novel dithiocarbamate-chalcone derivates

  • Bioorg Med Chem Lett. 2016 Aug 15;26(16):3918-22. doi: 10.1016/j.bmcl.2016.07.012.
Dong-Jun Fu 1,  Sai-Yang Zhang 1,  Ying-Chao Liu 1,  Li Zhang 1,  Jun-Ju Liu 1,  Jian Song 1,  Ruo-Han Zhao 1,  Feng Li 1,  Hui-Hui Sun 1,  Hong-Min Liu 1,  Yan-Bing Zhang 1
Affiliations

Affiliation

  • 1 Collaborative Innovation Center of New Drug Research and Safety Evaluation, School of Pharmaceutical Sciences, Zhengzhou University, Zhengzhou 450001, PR China.
PMID: 27423479 DOI: 10.1016/j.bmcl.2016.07.012
Abstract

A series of novel dithiocarbamate-chalcone derivates were designed, synthesized and evaluated for antiproliferative activity against three selected Cancer cell lines (EC-109, SK-N-SH and MGC-803). Majority of the synthesized compounds exhibited moderate to potent activity against all the Cancer cell lines assayed. Particularly, compounds II2 and II5 exhibited the excellent growth inhibition against SK-N-SH with IC50 values of 2.03μM and 2.46μM, respectively. Further mechanism studies revealed that compound II2 could obviously inhibit the proliferation of SK-N-SH cells by inducing Apoptosis and arresting the cell cycle at G0/G1 phase.

Keywords

Antiproliferative activity; Apoptosis; Chalcone; Dithiocarbamate.

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