Novel Nitric Oxide Donors of Phenylsulfonylfuroxan and 3-Benzyl Coumarin Derivatives as Potent Antitumor Agents

doi:10.1021/acsmedchemlett.8b00125

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	Novel Nitric Oxide Donors of Phenylsulfonylfuroxan and 3-Benzyl Coumarin Derivatives as Potent Antitumor Agents
	Guo, Yalan 1; Wang, Yujie 2; Li, Haihong 1; Wang, Ke 1; Wan, Qi 1; Li, Jia2 ; Zhou, Yubo2 ; Chen, Ying 1
刊名	ACS MEDICINAL CHEMISTRY LETTERS
	2018-05
卷号	9 期号:5 页码:502-506
关键词	Phenylsulfonylfuroxan 3-benzyl coumarin anticancer multidrug resistance P-gp overexpression
ISSN号	1948-5875
DOI	10.1021/acsmedchemlett.8b00125
文献子类	Article
英文摘要	In this work, five new hybrids of phenylsulfonylfuroxan merging 3-benzyl coumarin and their seco-B-ring derivatives 2-6 were designed and synthesized. Among them, compound 3 showed the most potent antiproliferation activities with IC50 values range from 0.5 to 143 nM against nine drug-sensitive and four drug-resistant cancer cell lines. Preliminary pharmacologic studies showed that these compounds displayed lower toxicities than that of lead compound 1. Compound 3 obviously induced the early apoptosis and hardly affected the cell cycle of A2780, which was significantly different from compound 1. Especially, it gave 559- and 294-fold selectivity antiproliferation activity in P-gp overexpressed drug-resistant cancer cell lines MCF-7/ADR and KB-V compared to their drug-sensitive ones MCF-7 and KB, implying that compounds 2-6 might have an extra mechanism of anti-MDR-cancer with P-gp overexpression.
资助项目	"Major New Drugs Innovation and Development" of National Science and Technology Major Projects[2018ZX09711002-007-005]
WOS关键词	DI-2-PYRIDYLKETONE 4,4-DIMETHYL-3-THIOSEMICARBAZONE DP44MT ; LYSOSOMAL P-GLYCOPROTEIN ; COLON-CANCER CELLS ; MULTIDRUG-RESISTANCE ; RAF/MEK INHIBITORS ; MECHANISM ; CHEMOSENSITIZATION ; PROLIFERATION ; CYTOTOXICITY ; DOXORUBICIN
WOS研究方向	Pharmacology & Pharmacy
语种	英语
出版者	AMER CHEMICAL SOC
WOS记录号	WOS:000432205400020
内容类型	期刊论文
源URL	[http://119.78.100.183/handle/2S10ELR8/279776]
专题	国家新药筛选中心中科院受体结构与功能重点实验室新药研究国家重点实验室药物安全性评价中心
通讯作者	Chen, Ying
作者单位	1.Fudan Univ, Sch Pharm, Dept Med Chem, Shanghai 201203, Peoples R China; 2.Chinese Acad Sci, Shanghai Inst Mat Med, State Key Lab Drug Res, Chinese Natl Ctr Drug Screening, Shanghai 201203, Peoples R China
推荐引用方式 GB/T 7714	Guo, Yalan,Wang, Yujie,Li, Haihong,et al. Novel Nitric Oxide Donors of Phenylsulfonylfuroxan and 3-Benzyl Coumarin Derivatives as Potent Antitumor Agents[J]. ACS MEDICINAL CHEMISTRY LETTERS,2018,9(5):502-506.
APA	Guo, Yalan.,Wang, Yujie.,Li, Haihong.,Wang, Ke.,Wan, Qi.,...&Chen, Ying.(2018).Novel Nitric Oxide Donors of Phenylsulfonylfuroxan and 3-Benzyl Coumarin Derivatives as Potent Antitumor Agents.ACS MEDICINAL CHEMISTRY LETTERS,9(5),502-506.
MLA	Guo, Yalan,et al."Novel Nitric Oxide Donors of Phenylsulfonylfuroxan and 3-Benzyl Coumarin Derivatives as Potent Antitumor Agents".ACS MEDICINAL CHEMISTRY LETTERS 9.5(2018):502-506.