| Literature DB >> 28785928 |
Dong-Jun Fu1,2,3,4, Ruo-Han Zhao1,2,3,4, Jia-Huan Li1,2,3,4, Jia-Jia Yang1,2,3,4, Ruo-Wang Mao1,2,3,4, Bo-Wen Wu1,2,3,4, Ping Li1,2,3,4, Xiao-Lin Zi5, Qing-Qing Zhang1,2,3,4, Hui-Jie Cai1,2,3,4, Sai-Yang Zhang6, Yan-Bing Zhang7,8,9,10, Hong-Min Liu11,12,13,14.
Abstract
Novel phenothiazine-dithiocarbamate analogues were designed by molecular hybridization strategy and synthesized and evaluated for their anticancer activity in vitro against three selected cancer cell lines (EC-109, MGC-803, and PC-3). The preliminary structure-activity relationship (SAR) for this phenothiazine-dithiocarbamate hybrids is explored. Among all analogues, 2-oxo-2-(10H-phenothiazin-10-yl)ethyl 4-ethylpiperazine-1-carbodithioate (8a) showed the most potent inhibitory activity with an [Formula: see text] value of [Formula: see text] against PC-3 cells. In addition, compound 8a could arrest the cell cycle at the G1 phase and regulate the expression of G1 checkpoint-related proteins, suggesting that phenothiazine-dithiocarbamate hybrids might be useful as cell cycle blockers.Entities:
Keywords: Antiproliferative activity; Dithiocarbamate; G1 checkpoint-related protein; G1 phase; Phenothiazine
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Year: 2017 PMID： 28785928 PMCID： PMC5975273 DOI： 10.1007/s11030-017-9773-4
Source DB: PubMed Journal: Mol Divers ISSN： 1381-1991 Impact factor: 2.943