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.
Click synthesis of a triazole-based inhibitor of Met functions in cancer cells / F. Colombo, C. Tintori, A. Furlan, S. Borrelli, M.S. Christodoulou, R. Dono, F. Maina, M. Botta, M. Amat, J. Bosch, D. Passarella. - In: BIOORGANIC & MEDICINAL CHEMISTRY LETTERS. - ISSN 0960-894X. - 22:14(2012), pp. 4693-4696.
Click synthesis of a triazole-based inhibitor of Met functions in cancer cells
S. Borrelli;M.S. Christodoulou;D. PassarellaUltimo
2012
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.File | Dimensione | Formato | |
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Bioorganic & Medicinal Chemistry Letters 22 (2012) 4693–4696.pdf
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