777096-61-4Relevant articles and documents
Synthesis of 1H-pyridin-2-one derivatives as potent and selective farnesyltransferase inhibitors
Wang, Le,Lin, Nan-Horng,Li, Qun,Henry, Rodger F.,Zhang, Haiying,Cohen, Jerome,Gu, Wen-Zhen,Marsh, Kennan C.,Bauch, Joy L.,Rosenberg, Saul H.,Sham, Hing L.
, p. 4603 - 4606 (2007/10/03)
The synthesis and biological evaluation of two novel series of potent and selective FTase inhibitors are described. Two novel series of potent and selective FTase inhibitors have been synthesized using structure-based design. Medicinal chemistry efforts led to the discovery of compound 4e with potent cellular activity and good oral bioavailability in dog. A synthetic route toward novel heterocycles 1,5-dimethyl-6-oxo-4-aryl-1,6-dihydro-pyridine-2- carbonitrile was established. The structure of compound 5c was confirmed by X-ray crystallography.