186202-60-8Relevant academic research and scientific papers
Dihydro-2h-napthalene-1-one inhibitors of ras farnesyl transferase
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Page 19, (2010/02/05)
The present invention provides dihydro-2H-napthalene-1-ones of formula (V), and pharmaceutically acceptable salts, esters, amides, and prodrugs thereof, which are useful for treating and preventing uncontrolled or abnormal proliferation of tissues, such a
Design and biological activity of (S)-4-(5-{[1-(3-Chlorobenzyl)-2-oxopyrrolidin-3-ylamino]methyl}imidazol-1- ylmethyl)benzonitrile, a 3-aminopyrrolidinone farnesyltransferase inhibitor with excellent cell potency
Bell,Gallicchio,Abrams,Beshore,Buser,Culberson,Davide,Ellis-Hutchings,Fernandes,Gibbs,Graham,Hartman,Heimbrook,Homnick,Huff,Kassahun,Koblan,Kohl,Lobell,Lynch Jr.,Miller,Omer,Rodrigues,Walsh,Williams
, p. 2933 - 2949 (2007/10/03)
The synthesis, structure-activity relationships, and biological properties of a novel series of imidazole-containing inhibitors of farnesyltransferase are described. Starting from a 3-amino-pyrrolidinone core, a systematic series of modifications provided 5h, a non-thiol, non-peptide farnesyltransferase inhibitor with excellent bioavailability in dogs. Compound 5h was found to have an unusually favorable ratio of cell potency to intrinsic potency, compared with other known FTIs. It exhibited excellent potency against a range of tumor cell lines in vitro and showed full efficacy in the K-rasB transgenic mouse model.
