'Click' synthesis of a triazole-based inhibitor of Met functions in cancer cells

被引：37

作者：

Colombo, Francesco ^{[1
]}

Tintori, Cristina ^{[2
]}

Furlan, Alessandro ^{[3
]}

Borrelli, Stella ^{[1
]}

Christodoulou, Michael S. ^{[1
]}

Dono, Rosanna ^{[3
]}

Maina, Flavio ^{[3
]}

Botta, Maurizio ^{[2
]}

Amat, Mercedes ^{[4
,5
]}

Bosch, Joan ^{[4
,5
]}

Passarella, Daniele ^{[1
]}

机构：

[1] Univ Milan, Dipartimento Chim Organ & Ind, I-20133 Milan, Italy

[2] Univ Siena, Dipartimento Farmaco Chim Tecnol, I-53100 Siena, Italy

[3] Aix Marseille Univ, IBDML, CNRS, UMR 7288, F-13288 Marseille 09, France

[4] Univ Barcelona, Fac Pharm, Organ Chem Lab, E-08028 Barcelona, Spain

[5] Univ Barcelona, Inst Biomed IBUB, E-08028 Barcelona, Spain

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2012年 / 22卷 / 14期

关键词：

Click chemistry; Cu(I)-catalyzed; Inhibition of HGF-induced scattering; Anticancer compounds; RECEPTOR TYROSINE KINASE; HEPATOCYTE GROWTH-FACTOR; C-MET; GENETIC ALGORITHM; SURVIVAL; ROLES;

D O I：

10.1016/j.bmcl.2012.05.078

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

The use of Cu(I)-catalyzed azide-alkyne 1,3-dipolar cycloaddition permitted the synthesis of a new compound that is able to inhibit the HGF-induced scattering of MDCK (epithelial cells) and in vitro tumorigenesis of H1437 (non-small-cell lung cancer) and GTL-16 (human gastric carcinoma). In agreement with biochemical and biological results, docking studies within the ATP binding site of Met suggested for the new synthesized compound a binding mode similar to that of the active compound Triflorcas previously reported. (C) 2012 Elsevier Ltd. All rights reserved.

引用

页码：4693 / 4696

页数：4

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