1263285-52-4Relevant articles and documents
Quinazolines with intra-molecular hydrogen bonding scaffold (iMHBS) as PI3K/mTOR dual inhibitors
Liu, Kevin K.C.,Huang, Xiaojun,Bagrodia, Shubha,Chen, Jeffrey H.,Greasley, Samantha,Cheng, Hengmiao,Sun, Shaoxian,Knighton, Dan,Rodgers, Caroline,Rafidi, Kristina,Zou, Aihua,Xiao, Jiezhan,Yan, Shengyong
, p. 1270 - 1274 (2011/04/16)
Intra-molecular hydrogen bonding was introduced to the quinazoline motif to form a pseudo ring (intra-molecular H-bond scaffold, iMHBS) to mimic our previous published core structures, pyrido[2.3-D]pyrimidin-7-one and pteridinone, as PI3K/mTOR dual inhibitors. This design results in potent PI3K/mTOR dual inhibitors and the purposed intra-molecular hydrogen bonding structure is well supported by co-crystal structure in PI3Kγ enzyme. In addition, a novel synthetic route was developed for these analogs.