Title of article :
Synthesis of 5,6-Dihydro-11H-benzo[5,6]-cyclohepta[1,2-b]pyridin-11-ylidene)-1-piperidine-N-cyanoguanidine Derivatives as Inhibitors of Ras Farnesyl Protein Transferase
Author/Authors :
Alan B. Cooper، نويسنده , , Corey L. Strickland، نويسنده , , DR James Wang، نويسنده , , Jagdish Desai، نويسنده , , Paul Kirschmeier، نويسنده , , Robert Patton Leland، نويسنده , , W. Robert Bishop، نويسنده , , Patricia C. Weber، نويسنده , , V. Girijavallabhan، نويسنده ,
Abstract :
A series of novel N-cyanoguanidine tricyclic farnesyl protein transferase (FPT) inhibitors was prepared. Replacement of a piperidine amide-group with a N-cyanoguanidine functionality increased FPT activity. X-ray crystal structure determination of 42 complexed with FPT revealed differences in the interactions of the amide and N-cyanoguanidine groups with the protein.
