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

详细信息    查看全文

• 作者：Dong-Jun Fu^&dagger ; ; Sai-Yang Zhang^&dagger ; ; Ying-Chao Liu ; Li Zhang ; Jun-Ju Liu ; Jian Song ; Ruo-Han Zhao ; Feng Li ; Hui-Hui Sun ; Hong-Min Liu ; Yan-Bing Zhang
• 关键词：Chalcone ; Dithiocarbamate ; Antiproliferative activity ; Apoptosis
• 刊名：Bioorganic & Medicinal Chemistry Letters
• 出版年：2016
• 出版时间：15 August 2016
• 年：2016
• 卷：26
• 期：16
• 页码：3918-3922
• 全文大小：1161 K

文摘

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 2.03 μM and 2.46 μM, 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.