吩噻嗪类化合物的分子多样性：作为潜在细胞周期阻断剂的吩噻嗪-二硫代氨基甲酸盐杂合体的设计与合成。
Molecular diversity of phenothiazines: design and synthesis of phenothiazine-dithiocarbamate hybrids as potential cell cycle blockers.
机构信息
New Drug Research and Development Center, School of Pharmaceutical Sciences, Zhengzhou University, Zhengzhou, 450001, China.
Collaborative Innovation Center of New Drug Research and Safety Evaluation, Henan Province, China.
出版信息
Mol Divers. 2017 Nov;21(4):933-942. doi: 10.1007/s11030-017-9773-4. Epub 2017 Aug 7.
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.
新型吩噻嗪-二硫代氨基甲酸盐类似物通过分子杂交策略设计、合成，并在体外对三种选定的癌细胞系（EC-109、MGC-803 和 PC-3）进行抗癌活性评估。初步探索了该吩噻嗪-二硫代氨基甲酸盐杂合体的结构-活性关系（SAR）。在所有类似物中，2-氧代-2-（10H-吩噻嗪-10-基）乙基 4-乙基哌嗪-1-碳二硫代酸酯（8a）对 PC-3 细胞的抑制活性最强，IC50 值为[Formula: see text]。此外，化合物 8a 可以将细胞周期阻滞在 G1 期，并调节 G1 检验点相关蛋白的表达，这表明吩噻嗪-二硫代氨基甲酸盐杂合体可能可用作细胞周期阻断剂。
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