1013099-80-3Relevant articles and documents
Structure-based design, SAR analysis and antitumor activity of PI3K/mTOR dual inhibitors from 4-methylpyridopyrimidinone series
Cheng, Hengmiao,Hoffman, Jacqui E.,Le, Phuong T.,Pairish, Mason,Kania, Robert,Farrell, William,Bagrodia, Shubha,Yuan, Jing,Sun, Shaoxian,Zhang, Eric,Xiang, Cathy,Dalvie, Deepak,Rahavendran, Sadayappan V.
supporting information, p. 2787 - 2792 (2013/07/04)
PI3K, AKT and mTOR, key kinases from a frequently dysregulated PI3K signaling pathway, have been extensively pursued to treat a variety of cancers in oncology. Clinical trials of PF-04691502, a highly potent and selective ATP competitive kinase inhibitor of class 1 PI3Ks and mTOR, from 4-methylpyridopyrimidinone series, led to the discovery of a metabolite with a terminal carboxylic acid, PF-06465603. This paper discusses structure-based drug design, SAR and antitumor activity of the MPP derivatives with a terminal alcohol, a carboxylic acid or a carboxyl amide.