Title of article :
Inhibitors of farnesyl protein transferase. synthesis and biological activity of amide and cyanoguanidine derivatives containing a 5,11-dihydro[1]benzthiepin, benzoxepin, and benzazepin [4,3-b]pyridine ring system
Author/Authors :
Ronald Wolin، نويسنده , , Michael Connolly، نويسنده , , Joseph Kelly، نويسنده , , Jay Weinstein، نويسنده , , Stuart Rosenblum، نويسنده , , Adriano Afonso، نويسنده , , Linda James-Myers، نويسنده , , Paul Kirschmeier، نويسنده , , W. Robert Bishop، نويسنده ,
Abstract :
Bioisosteric replacement of the C-6 carbon atom in piperidine I and piperazine II with S, O, and N heteroatoms is described. Amide and cyanoguanidine derivatives of these compounds were evaluated in vitro and found to be good inhibitors of farnesyl-protein transferase. An improved method of preparing the 5,11-dihydro-[1]-benzthiepin nucleus 6 was accomplished in high yield and with excellent regioselectivity using an AlCl3 melt protocol.
