Design,synthesis and preliminary antiproliferative activity studies of new diheteroaryl thioether derivatives |
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Authors: | Zhong-Hua Li Xue-Qi Liu Tao-Qian Zhao Peng-Fei Geng Ying Liu Bing Zhao Wen-Ge Guo Bin Yu Hong-Min Liu |
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Institution: | Collaborative Innovation Center of New Drug Research and Safety Evaluation, Henan Province, PR China;Key Laboratory of Technology of Drug Preparation (Zhengzhou University), Ministry of Education of China, PR China;Key Laboratory of Henan Province for Drug Quality and Evaluation; School of Pharmaceutical Sciences, Zhengzhou University, Zhengzhou 450001, PR China |
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Abstract: | A series of structurally new diheteroaryl thioether analogs was designed, prepared and screened toward MGC-803, MKN-45, EC-109 and H1650. Most of the target compounds displayed moderate to potent antiproliferative activities. Among them, compound 5 showed the best antiproliferative activity against the tested cell lines with the half maximal inhibitory concentration (IC50) values below 10 μM. In addition, flow cytometry analysis showed that compound 5 increased Bax expression, down-regulated expression of Bcl-2, cleaved caspases-3/9, finally inducing apoptosis of MKN-45 cells as well as arrested the cell cycle at G2/M phase. This study suggests that the diheteroaryl thioethers are a class of emerging chemotypes for developing antitumor agents or biological probes, and compound 5 could serve as a good starting point to design new apoptosis inducers. |
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Keywords: | Diheteroaryl thioether Antiproliferative activity Apoptosis Cell cycle arrest |
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