871357-90-3Relevant articles and documents
Development and scale-up of an optimized route to the ALK inhibitor CEP-28122
Allwein, Shawn P.,Roemmele, Renee C.,Haley, James J.,Mowrey, Dale R.,Petrillo, Daniel E.,Reif, James J.,Gingrich, Diane E.,Bakale, Roger P.
, p. 148 - 155 (2012/05/20)
Evolution of the process strategies to prepare CEP-28122, an anaplastic lymphoma kinase (ALK) inhibitor, is presented. The initial medicinal chemistry route, used for the preparation of key supplies for biological screening, is reviewed. In addition, the
Pyrazole diaminopyrimidines as dual inhibitors of KDR and Aurora B kinases
Curtin, Michael L.,Robin Heyman,Frey, Robin R.,Marcotte, Patrick A.,Glaser, Keith B.,Jankowski, James R.,Magoc, Terrance J.,Albert, Daniel H.,Olson, Amanda M.,Reuter, David R.,Bouska, Jennifer J.,Montgomery, Debra A.,Palma, Joann P.,Donawho, Cherrie K.,Stewart, Kent D.,Tse, Chris,Michaelides, Michael R.
scheme or table, p. 4750 - 4755 (2012/08/07)
In an effort to identify kinase inhibitors with dual KDR/Aurora B activity and improved aqueous solubility compared to the Abbott dual inhibitor ABT-348, a series of novel pyrazole pyrimidines structurally related to kinase inhibitor AS703569 were prepared. SAR work provided analogs with significant cellular activity, measureable aqueous solubility and moderate antitumor activity in a mouse tumor model after weekly ip dosing. Unfortunately these compounds were pan-kinase inhibitors that suffered from narrow therapeutic indices which prohibited their use as antitumor agents.
