Synthesis, antitumor activity and QSAR studies of some 4-aminomethylidene derivatives of edaravone

被引：20
|
作者：
Markovic, Violeta [1 ]
Eric, Slavica [2 ]
Juranic, Zorica D. [3 ]
Stanojkovic, Tatjana [3 ]
Joksovic, Ljubinka [1 ]
Rankovic, Branislav [4 ]
Kosanic, Marijana [4 ]
Joksovic, Milan D. [1 ]
机构：
[1] Univ Kragujevac, Fac Sci, Dept Chem, Kragujevac 34000, Serbia
[2] Univ Belgrade, Fac Pharm, Belgrade 11000, Serbia
[3] Inst Oncol & Radiol Serbia, Belgrade 11000, Serbia
[4] Univ Kragujevac, Fac Sci, Dept Biol, Kragujevac 34000, Serbia
来源：
BIOORGANIC CHEMISTRY | 2011年 / 39卷 / 1-3期
关键词：
Edaravone derivatives; Antitumor activity; QSAR studies; RAPID COLORIMETRIC ASSAY; INHIBITORS; PYRAZOLONES;
D O I：
10.1016/j.bioorg.2010.10.003
中图分类号：
Q5 [生物化学]; Q7 [分子生物学];
学科分类号：
071010 ; 081704 ;
摘要：
A series of aminomethylidene derivatives obtained from 4-formyledaravone were synthesized and characterized by IR, NMR and elemental analysis. All the compounds were screened for their antitumor activity. The compound containing 5-phenylpyrazole moiety (3q) exhibited remarkable antitumor activity in in vitro assays, especially against human breast cancer MDA-MB-361 and MDA-MB-453 cell lines. The most important whole-molecule descriptors for antitumor activity on MDA-MB-453 cells belong to the group of quantum-chemical descriptors. (C) 2010 Elsevier Inc. All rights reserved.
引用
收藏
页码：18 / 27
页数：10
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