Design, synthesis and antiproliferative activity studies of novel dithiocarbamate–chalcone derivates. Issue 16 (15th August 2016)

• Record Type: Journal Article
• Authors: Fu, Dong-Jun; Zhang, Sai-Yang; Liu, Ying-Chao; Zhang, Li; Liu, Jun-Ju; Song, Jian; Zhao, Ruo-Han; Li, Feng; Sun, Hui-Hui; Liu, Hong-Min; Zhang, Yan-Bing
• Is Part Of: Bioorganic & medicinal chemistry letters. Volume 26:Issue 16(2016)
• Page Start: 3918
• Page End: 3922
• Publication Date: 2016-08-15
• Subjects: Chalcone -- Dithiocarbamate -- Antiproliferative activity -- Apoptosis; Bioorganic chemistry -- Periodicals; Pharmaceutical chemistry -- Periodicals; 572
• DOI: 10.1016/j.bmcl.2016.07.012
• Languages: English
• ISSNs: 0960-894X

Abstract

Graphical 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, compoundsII2 andII5 exhibited the excellent growth inhibition against SK-N-SH with IC50 values of 2.03 μM and 2.46 μM, respectively. Further mechanism studies revealed that compoundII2 could obviously inhibit the proliferation of SK-N-SH cells by inducing apoptosis and arresting the cell cycle at G0/G1 phase. 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, compoundsII2 andII5 exhibited the excellent growth inhibition against SK-N-SH with IC50 values of 2.03 μM and 2.46 μM, respectively. Further mechanism studies revealed that compoundII2 could obviously inhibit the proliferation of SK-N-SH cells by inducing apoptosis and arresting the cell cycle at G0/G1 phase.