226930-29-6Relevant academic research and scientific papers
A novel class of highly potent, selective, and non-peptidic inhibitor of ras farnesyltransferase (FTase)
Lee, Hyunil,Lee, Jinho,Lee, Sangkyun,Shin, Youseung,Jung, Wonhee,Kim, Jong-Hyun,Park, Kiwon,Kim, Kwihwa,Cho, Heung Soo,Ro, Seonggu,Lee, Sunhwa,Jeong, ShinWu,Choi, Taesaeng,Chung, Hyun-Ho,Koh, Jong Sung
, p. 3069 - 3072 (2007/10/03)
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.
Imidazole derivatives having an inhibitory activity for farnesyl transferase and process for preparation thereof
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, (2008/06/13)
The present invention relates to a novel imidazole derivative represented by formula (1) which shows an inhibitory activity against farnesyl transferase or pharmaceutically acceptable salts or isomers thereof, in which A, n1and Y are defined in the specification; to a process for preparation of the compound of formula (1); to intermediates which are used in the preparation of the compound of formula (1); and to a pharmaceutical composition comprising the compound of formula (1) as an active ingredient.
