Synthesis and Cdc25B/PTP1B Inhibitory Activity Evaluation of Novel Acylhydrazone Derivatives Containing Carbazole Moity

doi:10.6023/cjoc201806042

	Synthesis and Cdc25B/PTP1B Inhibitory Activity Evaluation of Novel Acylhydrazone Derivatives Containing Carbazole Moity
	Li Yingjun 2; Wang Siyuan 2; Jin Kun 1; Gao Lixin 3; Sheng Li 3; Zhang Nan 2; Liu Jihong 4; Li Jia 3
刊名	CHINESE JOURNAL OF ORGANIC CHEMISTRY
	2019-02-25
卷号	39 期号:2 页码:491-499
关键词	acylhydrazone carbazole synthesis Cdc25B and PTP1B inhibitor molecular docking
ISSN号	0253-2786
DOI	10.6023/cjoc201806042
通讯作者	Li Yingjun(chemlab.lnnu@163.com) ; Li Jia()
英文摘要	A series of novel acylhydmzone derivatives 6 containing carbazole moity were synthesized by carbazole and 4-cyanobenzyl chloride as starting materials via multi-step reactions. Their structures were characterized by IR, H-1 NMR, C-13 NMR spectra and elemental analysis. All synthesized target compounds were evaluated for the inhibitory activities against Cdc25B and PTP1B. The results show that the target compounds display significant inhibitory activities against Cdc25B/PTP1B. Among them, compound 4-((carbazol-9-yl)methyl),N'-(2-hydroxy-1-naphthaleny hnethylene)benzoyl hydrazide (6g) had the highest inhibitory activities against Cdc25B and PTP1B with IC50 values of (2.16 +/- 0.38) and (1.06 +/- 0.23) mu g/mL, respectively. The molecular docking results indicated that the hydrogen bond and hydrophobic interaction formed between compound 6g and Cdc25B/PTP1B enzyme.
资助项目	Natural Science Foundation of Liaoning Province[20102126]
WOS关键词	BIOLOGICAL EVALUATION ; ANTITUBERCULOSIS ACTIVITY ; PHOSPHATASE INHIBITORS ; ANTIMICROBIAL ACTIVITY ; DOCKING ; OPTIMIZATION ; MECHANISM ; ANALOGS ; DESIGN ; AGENTS
WOS研究方向	Chemistry
语种	英语
出版者	SCIENCE PRESS
WOS记录号	WOS:000458607700023
内容类型	期刊论文
源URL	[http://119.78.100.183/handle/2S10ELR8/290485]
专题	中国科学院上海药物研究所
通讯作者	Li Yingjun; Li Jia
作者单位	1.Dalian Univ Technol, State Key Lab Fine Chem, Dalian 116012, Peoples R China 2.Liaoning Normal Univ, Coll Chem & Chem Engn, Dalian 116029, Peoples R China 3.Chinese Acad Sci, State Key Lab Drug Res, Natl Ctr Drug Screening, Shanghai Inst Mat Med, Shanghai 201203, Peoples R China 4.Dalian Univ Technol, Chem Anal & Res Ctr, Fac Chem Environm & Biol Sci & Technol, Dalian 116023, Peoples R China
推荐引用方式 GB/T 7714	Li Yingjun,Wang Siyuan,Jin Kun,et al. Synthesis and Cdc25B/PTP1B Inhibitory Activity Evaluation of Novel Acylhydrazone Derivatives Containing Carbazole Moity[J]. CHINESE JOURNAL OF ORGANIC CHEMISTRY,2019,39(2):491-499.
APA	Li Yingjun.,Wang Siyuan.,Jin Kun.,Gao Lixin.,Sheng Li.,...&Li Jia.(2019).Synthesis and Cdc25B/PTP1B Inhibitory Activity Evaluation of Novel Acylhydrazone Derivatives Containing Carbazole Moity.CHINESE JOURNAL OF ORGANIC CHEMISTRY,39(2),491-499.
MLA	Li Yingjun,et al."Synthesis and Cdc25B/PTP1B Inhibitory Activity Evaluation of Novel Acylhydrazone Derivatives Containing Carbazole Moity".CHINESE JOURNAL OF ORGANIC CHEMISTRY 39.2(2019):491-499.