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Deprecated: Implicit conversion from float 265.2 to int loses precision in C:\Inetpub\vhosts\kidney.de\httpdocs\pget.php on line 534 ACS+Med+Chem+Lett 2012 ; 3 (12): 997-1002 Nephropedia Template TP
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Discovery of AC710, a Globally Selective Inhibitor of Platelet-Derived Growth Factor Receptor-Family Kinases #MMPMID24900421
Liu G; Campbell BT; Holladay MW; Ford Pulido JM; Hua H; Gitnick D; Gardner M; James J; Breider MA; Brigham D; Belli B; Armstrong R; Treiber DK
ACS Med Chem Lett 2012[Dec]; 3 (12): 997-1002 PMID24900421show ga
A series of potent, selective platelet-derived growth factor receptor-family kinase inhibitors was optimized starting from a globally selective lead molecule 4 through structural modifications aimed at improving the physiochemical and pharmacokinetic properties, as exemplified by 18b. Further clearance reduction via per-methylation of the ?-carbons of a solubilizing piperidine nitrogen resulted in advanced leads 22a and 22b. Results from a mouse tumor xenograft, a collagen-induced arthritis model, and a 7 day rat in vivo tolerability study culminated in the selection of compound 22b (AC710) as a preclinical development candidate.