893420-25-2Relevant academic research and scientific papers
Imidazole pyrimidine amides as potent, orally bioavailable cyclin-dependent kinase inhibitors
Jones, Clifford D.,Andrews, David M.,Barker, Andrew J.,Blades, Kevin,Byth, Kate F.,Finlay, M. Raymond V.,Geh, Catherine,Green, Clive P.,Johannsen, Marie,Walker, Mike,Weir, Hazel M.
scheme or table, p. 6486 - 6489 (2009/10/01)
The development of a novel series of imidazole pyrimidine amides as cyclin-dependent kinase (CDK) inhibitors is described. The series was found to have much improved CDK2 inhibition and potent in vitro anti-proliferative effects against cancer cell lines. Control of overall lipophilicity was important to achieve good in vitro potency along with acceptable physiochemical properties and margins against inhibition of both CYP isoforms and the hERG potassium ion channel. A compound with an attractive overall balance of properties was profiled in vivo and possessed suitable physiochemical and pharmacokinetic profiles for oral dosing.
4- (4- (IMIDAZOL-4-YL) PYRIMIDIN-2-YLAMINO) BENZAMIDES AS CDK INHIBITORS
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Page/Page column 67, (2008/06/13)
Compounds of the formula: (I): wherein variable groups are as defined within and a pharmaceutically acceptable salts and in vivo hydrolysable esters are described. Also described are processes for their preparation and their use as medicaments, particularly medicaments for producing a cell cycle inhibitory (anti-cell-proliferation) effect in a warm-blooded animal, such as man.
