A series of novel sorafenib derivatives containing quinazoline moiety were designed and synthesized. Their anti-proliferative activities against HCT116 and HCT115 cell lines were evaluated using MTT assay. Most of the...A series of novel sorafenib derivatives containing quinazoline moiety were designed and synthesized. Their anti-proliferative activities against HCT116 and HCT115 cell lines were evaluated using MTT assay. Most of the synthesized compounds showed significant cytotoxicity against the selected cell lines. These cytotoxicities were consistent with their inhibitory activity against the phosphorylation of c-Raf, MEK1/2 and ERK1/2. Compound GD-09 also showed much stronger anti-tumor activity than that of sorafenib in vivo by B16 melanoma xenograft model test.展开更多
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...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.展开更多
Two new series of diaryl thiourea containing sorafenib derivatives 9a-9t were designed and synthesized, and their antiproliferative activities against PC-3, HCT116 and MDA-MB-231 cell lines were evaluated. All compoun...Two new series of diaryl thiourea containing sorafenib derivatives 9a-9t were designed and synthesized, and their antiproliferative activities against PC-3, HCT116 and MDA-MB-231 cell lines were evaluated. All compounds generally showed antiproliferative activity to PC-3 cells, most of the analogs exhibited potent antiproliferative ac- tivity to HCT116 cells, and compounds 9e, 9f, 9o and 9p demonstrated inhibitory activities against all three cell lines. The structures of all the newly synthesized compounds were determined by JH NMR, 13C NMR and HRMS.展开更多
基金Supported by the National Natural Science Foundation of China(81202038)Science and Technology Innovation Foundation in Yantai University(01081)
文摘A series of novel sorafenib derivatives containing quinazoline moiety were designed and synthesized. Their anti-proliferative activities against HCT116 and HCT115 cell lines were evaluated using MTT assay. Most of the synthesized compounds showed significant cytotoxicity against the selected cell lines. These cytotoxicities were consistent with their inhibitory activity against the phosphorylation of c-Raf, MEK1/2 and ERK1/2. Compound GD-09 also showed much stronger anti-tumor activity than that of sorafenib in vivo by B16 melanoma xenograft model test.
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）.
文摘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.
文摘Two new series of diaryl thiourea containing sorafenib derivatives 9a-9t were designed and synthesized, and their antiproliferative activities against PC-3, HCT116 and MDA-MB-231 cell lines were evaluated. All compounds generally showed antiproliferative activity to PC-3 cells, most of the analogs exhibited potent antiproliferative ac- tivity to HCT116 cells, and compounds 9e, 9f, 9o and 9p demonstrated inhibitory activities against all three cell lines. The structures of all the newly synthesized compounds were determined by JH NMR, 13C NMR and HRMS.
