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. Passarella
Ultimo
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.
anticancer compounds; click chemistry; Cu(I)-catalyzed; Inhibition of HGF-induced scattering
Settore CHIM/06 - Chimica Organica
2012
Article (author)
File in questo prodotto:
File Dimensione Formato  
Bioorganic & Medicinal Chemistry Letters 22 (2012) 4693–4696.pdf

accesso riservato

Tipologia: Publisher's version/PDF
Dimensione 497.54 kB
Formato Adobe PDF
497.54 kB Adobe PDF   Visualizza/Apri   Richiedi una copia
Pubblicazioni consigliate

I documenti in IRIS sono protetti da copyright e tutti i diritti sono riservati, salvo diversa indicazione.

Utilizza questo identificativo per citare o creare un link a questo documento: https://hdl.handle.net/2434/191835
Citazioni
  • ???jsp.display-item.citation.pmc??? 8
  • Scopus 35
  • ???jsp.display-item.citation.isi??? 33
social impact