219862-37-0Relevant articles and documents
Design, synthesis, and structure-activity relationships of tetrahydroquinoline-based farnesyltransferase inhibitors
Lombardo, Louis J.,Camuso, Amy,Clark, John,Fager, Krista,Gullo-Brown, Johnni,Hunt, John T.,Inigo, Ivan,Kan, David,Koplowitz, Barry,Lee, Francis,McGlinchey, Kelly,Qian, Ligang,Ricca, Carolyn,Rovnyak, George,Traeger, Sarah,Tokarski, John,Williams, David K.,Wu, Laurence I.,Zhao, Yufen,Manne, Veeraswamy,Bhide, Rajeev S.
, p. 1895 - 1899 (2005)
Tetrahydroquinoline-based small molecule inhibitors of farnesyltransferase (FT) have been identified. Lead compounds were shown to have nanomolar to sub-nanomolar activity in biochemical assays with excellent potency in a Ras-mutated cellular reversion as
Inhibitors of farnesyl protein transferase
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, (2008/06/13)
Disclosed are quinoline and benzazepine derivatives that inhibit farnesyl-protein transferase (FTase) and the farnesylation of the oncogenic protein Ras. Thus, the compounds are useful as anti-cancer agents. The compounds are also useful in the treatment of diseases other than cancer.
