Synthesis and antiproliferative activities of N-(naphthalen-2-yl)acetamide and N-(substituted phenyl)acetamide bearing quinolin-2(1H)-one and 3,4-dihydroquinolin-2(1H)-one derivatives

被引：14

作者：

Chen, I-Li ^{[1
]}

Chen, Jih-Jung ^{[1
]}

Lin, Yu-Chin ^{[2
]}

Peng, Ching-Tien ^{[3
,4
,5
]}

Juang, Shin-Hun ^{[6
,7
]}

Wang, Tai-Chi ^{[1
]}

机构：

[1] Tajen Univ, Dept Pharm, Pingtung, Taiwan

[2] China Med Univ, Coll Pharm, Taichung, Taiwan

[3] China Med Univ, Sch Chinese Med, Taichung, Taiwan

[4] China Med Univ Hosp, Childrens Hosp, Dept Pediat, Taichung, Taiwan

[5] Asia Univ, Dept Biotechnol, Taichung, Taiwan

[6] China Med Univ, Grad Inst Pharmaceut Chem, Taichung, Taiwan

[7] China Med Univ Hosp, Dept Med Res, Taichung, Taiwan

来源：

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY | 2013年 / 59卷

关键词：

Quinolin-2(1H)-one; 3,4-Dihydroquinolin-2(1H)-one; Nasopharyngeal carcinoma; Antiproliferative activity; METHYLIDENE-GAMMA-BUTYROLACTONES; POSITIVE INOTROPIC AGENTS; NASOPHARYNGEAL CARCINOMA; ANTIPLATELET ACTIVITIES; BIOLOGICAL EVALUATION; INHIBITORS; DESIGN;

D O I：

10.1016/j.ejmech.2012.11.016

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Certain N-(naphthalen-2-yl)acetamide and N-( substituted phenyl)acetamide bearing quinolin-2(1H)-one and 3,4-dihydroquinolin-2(1H)-one derivatives have been synthesized and evaluated in vitro for their antiproliferative activities against a panel of human cancer cell lines including nasopharyngeal (NPC-TW01), lung carcinoma (H661), hepatoma (Hep3B), renal carcinoma (A498), and gastric cancer (MKN45). Among them, N-(naphthalen-2-yl)-2-(2-oxo-1,2,3,4-tetrahydroquinolin-6-yloxy)acetamide (18) was the most active against NPC-TW01 with an IC50 value of 0.6 mu M. Studies on NPC-TW01 cell cycle distribution revealed that compound 18 inhibited proliferation of NPC-TW01 by the alteration of cell division, accumulation of cells in S phase in a time- and concentration-dependent manners. In addition, compound 18 demonstrated very specific cytotoxicity against human nasopharyngeal carcinoma (NPC-TW01) cell lines with no detectable cytotoxicity against peripheral blood mononuclear cells (PBMCs) at a concentration of up to 50 mu M. (C) 2012 Elsevier Masson SAS. All rights reserved.

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页码：227 / 234

页数：8

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