2. Academic Validation
  3. 'Click' synthesis of a triazole-based inhibitor of Met functions in cancer cells

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

  • Bioorg Med Chem Lett. 2012 Jul 15;22(14):4693-6. doi: 10.1016/j.bmcl.2012.05.078.
Francesco Colombo 1,  Cristina Tintori,  Alessandro Furlan,  Stella Borrelli,  Michael S Christodoulou,  Rosanna Dono,  Flavio Maina,  Maurizio Botta,  Mercedes Amat,  Joan Bosch,  Daniele Passarella
Affiliations

Affiliation

  • 1 Dipartimento di Chimica Organica e Industriale, Università degli Studi di Milano, Via Venezian 21, 20133 Milano, Italy.
PMID: 22738633 DOI: 10.1016/j.bmcl.2012.05.078
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.

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