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Design and Synthesis of Hydrazine and Oxadiazole-containing Derivatives of Sorafenib as Antitumor Agents

Design and Synthesis of Hydrazine and Oxadiazole-containing Derivatives of Sorafenib as Antitumor Agents
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摘要 A series of hydrazine and oxadiazole analogs of Sorafenib was designed, synthesized and characterized by proton nuclear magnetic resonance(1H NMR) spectrometry and high resolution mass spectrometry(HRMS). The anti-proliferative activities of these compounds against human colorectal earcinoma(HCT-116) and human breast cancer (MDA-MB-231) tumor cell lines were evaluated in vitro by MTT method[MTT=3-(4,5-dimethylthiazol-2-yl)-2,5- diphenyltetrazolium bromide]. The bioassay results suggest that most of the synthesized compounds have antitumor potential to HCT-116 cell line compared with MDA-MB-231 cell line. Compounds 8a, 8b, 8d, Be, 9f and 9j competitive with Sorafenib demonstrated antiproliferative activities on HCT-116 cell line. A series of hydrazine and oxadiazole analogs of Sorafenib was designed, synthesized and characterized by proton nuclear magnetic resonance(1H NMR) spectrometry and high resolution mass spectrometry(HRMS). The anti-proliferative activities of these compounds against human colorectal earcinoma(HCT-116) and human breast cancer (MDA-MB-231) tumor cell lines were evaluated in vitro by MTT method[MTT=3-(4,5-dimethylthiazol-2-yl)-2,5- diphenyltetrazolium bromide]. The bioassay results suggest that most of the synthesized compounds have antitumor potential to HCT-116 cell line compared with MDA-MB-231 cell line. Compounds 8a, 8b, 8d, Be, 9f and 9j competitive with Sorafenib demonstrated antiproliferative activities on HCT-116 cell line.
出处 《Chemical Research in Chinese Universities》 SCIE CAS CSCD 2013年第3期454-459,共6页 高等学校化学研究(英文版)
基金 Supported by the National Natural Science Foundation of China(No.21072115) and the Student Training Programs for Innovation of Shandong University, China(No.201210422076).
关键词 Sorafenib analog Antiproliferative activity Antitumor agent Sorafenib analog Antiproliferative activity Antitumor agent
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