Oxime-based inhibitors of glucose transporter 1 displaying antiproliferative effects in cancer cells.
Tuccinardi T, Granchi C, Iegre J, Paterni I, Bertini S, Macchia M, Martinelli A, Qian Y, Chen X, Minutolo F.
An analysis of the main pharmacophoric features present in the still limited number of inhibitors of glucose transporter GLUT1 led to the identification of new oxime-based inhibitors, which proved to be able to efficiently hinder glucose uptake and cell growth in H1299 lung cancer cells. The most important interactions of a representative inhibitor were indicated by a novel computational model of GLUT1, which was purposely developed to explain these results and to provide useful indications for the design and the development of new and more efficient GLUT1 inhibitors.