Synthesis and antiproliferative activity of some 3-(pyrid-2-yl)-pyrazolines

被引：30
|
作者：
Ciupa, Alexander [1 ]
De Bank, Paul A. [1 ]
Mahon, Mary F. [2 ]
Wood, Pauline J. [1 ]
Caggiano, Lorenzo [1 ]
机构：
[1] Univ Bath, Dept Pharm & Pharmacol, Bath BA2 7AY, Avon, England
[2] Univ Bath, Dept Chem, Xray Crystallog Unit, Bath BA2 7AY, Avon, England
来源：
MEDCHEMCOMM | 2013年 / 4卷 / 06期
关键词：
SELECTIVE INHIBITORY-ACTIVITY; MAO-B INHIBITORS; MONOAMINE-OXIDASE; TUBULIN POLYMERIZATION; 1-ACETYL-3,5-DIPHENYL-4,5-DIHYDRO-(1H)-PYRAZOLE DERIVATIVES; BIOLOGICAL EVALUATION; PYRAZOLE DERIVATIVES; ANTICANCER ACTIVITY; ANTITUMOR-ACTIVITY; AGENTS;
D O I：
10.1039/c3md00077j
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：
The synthesis and antiproliferative activity of eleven 3-(pyrid-2-yl)-pyrazolines in two cancer cell lines are reported. X-ray crystallography was obtained of the lead compound 8i which was screened in the NCI 60 human tumour cell line and displayed sub-micromolar activity. Cell cycle analysis, in vitro tubulin assay and confocal microscopy are also reported and suggest that the lead compound disrupts microtubule formation.
引用
收藏
页码：956 / 961
页数：6
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