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Discovery of Novel Tricyclic 5H-Pyridazino4,5-bindoles as Potent Antitumor Agents: Design, Synthesis and Biological Evaluation
Alternative TitleDiscovery of Novel Tricyclic 5H-Pyridazino4,5-bindoles as Potent Antitumor Agents: Design,Synthesis and Biological Evaluation
Zhai Xin; Wang Limei; Shi Jiyue; Gong Ping
2015
Source PublicationCHEMICAL RESEARCH IN CHINESE UNIVERSITIES
ISSN1005-9040
Volume31Issue:3Pages:372-380
AbstractA novel series of 5H-pyridazino4,5-bindoles(L-01-L-32) was synthesized and characterized by means of H-1 NMR, MS and elemental analysis. The cytotoxicity of the target compounds against Bel-7402 and HT-1080 cell lines were evaluated by 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide(MTT) assay. Most of them exhibited moderate to excellent cytotoxicity, and six compounds(L-04, L-06, L-18, L-20, L-21 and L-23) possessed dramatically increased cytotoxicity superior to Gefitinib. Of these initial hits, compound L-21 displayed remarkable cytotoxicity against the tested cell lines with half maximal inhibitory concentration(IC50) values of 4.6 and 2.1 mu mol/L, respectively, which was 13.9- to 25.6-fold more potent than positive control.
Other AbstractA novel series of 5H-pyridazino4,5-bindoles(L-01-L-32) was synthesized and characterized by means of ~1H NMR, MS and elemental analysis. The cytotoxicity of the target compounds against Bel-7402 and HT-1080 cell lines were evaluated by 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide(MTT) assay. Most of them exhibited moderate to excellent cytotoxicity, and six compounds(L-04, L-06, L-18, L-20, L-21 and L-23) possessed dramatically increased cytotoxicity superior to Gefitinib. Of these initial hits, compound L-21 displayed remarkable cytotoxicity against the tested cell lines with half maximal inhibitory concentration(IC_(50)) values of 4.6 and 2.1 μmol/L, respectively, which was 13.9- to 25.6-fold more potent than positive control.
KeywordTYROSINE KINASE INHIBITORS GROWTH-FACTOR RECEPTOR ANALOGS DERIVATIVES BINDING HARMINE 1-Anilino-5H-pyridazino4,5-bindole EGFR inhibitor Cytotoxicity
Indexed ByCSCD
Language英语
Funding Project[National Natural Science Foundation of China] ; [Liaoning Baiqianwan Talents Program, China]
CSCD IDCSCD:5434854
Citation statistics
Cited Times:2[CSCD]   [CSCD Record]
Document Type期刊论文
Identifierhttp://ir.imr.ac.cn/handle/321006/150263
Collection中国科学院金属研究所
Affiliation中国科学院金属研究所
Recommended Citation
GB/T 7714
Zhai Xin,Wang Limei,Shi Jiyue,et al. Discovery of Novel Tricyclic 5H-Pyridazino4,5-bindoles as Potent Antitumor Agents: Design, Synthesis and Biological Evaluation[J]. CHEMICAL RESEARCH IN CHINESE UNIVERSITIES,2015,31(3):372-380.
APA Zhai Xin,Wang Limei,Shi Jiyue,&Gong Ping.(2015).Discovery of Novel Tricyclic 5H-Pyridazino4,5-bindoles as Potent Antitumor Agents: Design, Synthesis and Biological Evaluation.CHEMICAL RESEARCH IN CHINESE UNIVERSITIES,31(3),372-380.
MLA Zhai Xin,et al."Discovery of Novel Tricyclic 5H-Pyridazino4,5-bindoles as Potent Antitumor Agents: Design, Synthesis and Biological Evaluation".CHEMICAL RESEARCH IN CHINESE UNIVERSITIES 31.3(2015):372-380.
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