Novel tricyclic aminoacetyl and sulfonamide inhibitors of ras farnesyl protein transferase
Novel tricyclic FPT inhibitors with submicromolar FPT activity are described. Greatly enhanced FPT activity is realized with phthaloyl derivatized amino compound 2k, which showed FPT inhibitory activity of IC50 = 0.66 μM. Sulfonamides 5g and 50 were also found to be potent FPT inhibitor. SAR resulting from a variety of tricyclic amino acids and sulfonamide derivatives is discussed.
Njoroge, F. George,Vibulbhan, Bancha,Alvarez, Carmen S.,Bishop, W. Robert,Petrin, Joanne,Doll, Ronald J.,Girijavallabhan,Ganguly, Ashit K.
Get Best Price for183741-33-5[(R)-2-[4-(8-Chloro-5,6-dihydro-benzo[5,6]cyclohepta[1,2-b]pyridin-11-ylidene)-piperidin-1-yl]-1-(4-methoxy-benzylsulfanylmethyl)-2-oxo-ethyl]-carbamic acid tert-butyl ester