Synthesis and in vitro antitumor activity of novel naphthyridinone derivatives

被引：48

作者：

Jia, Xue-Dong ^{[1
,2
,3
]}

Wang, Shuo ^{[1
,2
]}

Wang, Ming-Hua ^{[1
,2
]}

Liu, Ming-Liang ^{[1
,2
]}

Xia, Gui-Min ^{[1
,2
]}

Liu, Xiu-Jun ^{[1
,2
]}

Chai, Yun ^{[1
,2
]}

He, Hong-Wei ^{[1
,2
]}

机构：

[1] Chinese Acad Med Sci, Inst Med Biotechnol, Beijing 100050, Peoples R China

[2] Peking Union Med Coll, Beijing 100050, Peoples R China

[3] Zhengzhou Univ, Affiliated Hosp 1, Zhengzhou 450052, Peoples R China

来源：

CHINESE CHEMICAL LETTERS | 2017年 / 28卷 / 02期

关键词：

Naphthyridinones; Synthesis; Antitumor activity; Voreloxin; 7-SUBSTITUTED 1,4-DIHYDRO-4-OXO-1-(2-THIAZOLYL)-1,8-NAPHTHYRIDINE-3-CARBOXYLIC ACIDS; ANTIBACTERIAL ACTIVITY; FLUOROQUINOLONE DERIVATIVES; ANTIMYCOBACTERIAL; AGENTS; DRUGS;

D O I：

10.1016/j.cclet.2016.07.024

中图分类号：

O6 [化学];

学科分类号：

0703 ;

摘要：

A series of naphthyridinone derivatives based on 1a (a precursor of Voreloxin) were designed and synthesized. Seven compounds having >70% inhibition against HL60 at 30 mu mol/L were further evaluated for their in vitro antitumor activity by SRB assay. Results reveal that thiazol-2-y1 and 3-aminomethyl-4-benzyloxyimino-3-methylpyrrolidin-1-yl groups are optimal at the N-1 and C-7 positions of naphthyridinone core, respectively. 10j exhibits broad-spectrum activity (IC50: <0.5-6.25 mu mol/L) against all of the tested cell lines including Etoposide- and/or 1a-resistant ones, and is 1.3-fold to >100-fold more potent than the two references against eight Of these cell lines. (C) 2016 Chinese Chemical Society and Institute of Materia Medica, Chinese Academy of Medical Sciences. Published by Elsevier B.V. All rights reserved.

引用

页码：235 / 239

页数：5

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