2013年1月7日星期一

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

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

Bioorg Med Chem Lett. 2012 Jul 15;22(14):4693-6

Authors: Colombo F, Tintori C, Furlan A, Borrelli S, Christodoulou MS, Dono R, Maina F, Botta M, Amat M, Bosch J, Passarella D

Abstract
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.

PMID: 22738633 [PubMed - indexed for MEDLINE]

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