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Discovery of Novel Tricyclic 5H-Pyridazino[4,5-b]indoles as Potent Antitumor Agents: Design,Synthesis and Biological Evaluation

Zhai Xin Wang Limei Shi Jiyue Gong Ping ^*

文摘	A novel series of 5H-pyridazino[4,5-b]indoles(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.
来源	Chemical Research in Chinese Universities ,2015,31(3):372-380 【核心库】
DOI	10.1007/s40242-015-4435-5
关键词	l-Anilino-5H-pyridazino[4,5-b]indole ; EGFR inhibitor ; Cytotoxicity
地址	Shenyang Pharmaceutical University, Key Laboratory of Structure-based Drug Design and Discovery, Ministry of Education, Shenyang, 110016
语种	英文
文献类型	研究性论文
ISSN	1005-9040
学科	化学
基金	国家自然科学基金 ; the Liaoning Baiqianwan Talents Program, China
文献收藏号	CSCD:5434854

参考文献共 14 共1页

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