Title of article :
A novel class of highly potent, selective, and non-peptidic inhibitor of ras farnesyltransferase (FTase)
Author/Authors :
Hyunil Lee، نويسنده , , Jinho Lee، نويسنده , , Sangkyun Lee، نويسنده , , Youseung Shin، نويسنده , , Wonhee Jung، نويسنده , , Jong-Hyun Kim، نويسنده , , Kiwon Park، نويسنده , , Kwihwa Kim، نويسنده , , Heung Soo Cho، نويسنده , , Seonggu Ro، نويسنده , , Sunhwa Lee، نويسنده , , ShinWu Jeong، نويسنده , , Taesaeng Choi، نويسنده , , Hyun-Ho Chung، نويسنده , , Jong Sung Koh، نويسنده ,
Abstract :
Design, synthesis and structure–activity relationship of a class of aryl pyrroles as farnesyltransferase inhibitors are described. In vitro and in vivo evaluation of a panel of these inhibitors led to identification of 2 (LB42908) as a highly potent (IC50=0.9 nM against H-Ras and 2.4 nM against K-Ras) antitumor agent that is currently undergoing preclinical studies.
