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

页码：956 / 961

页数：6

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