Download MendeleyQuinazolines with intra-molecular hydrogen bonding scaffold (iMHBS) as PI3K/mTOR dual inhibitors.
Liu, K.K., Huang, X., Bagrodia, S., Chen, J.H., Greasley, S., Cheng, H., Sun, S., Knighton, D., Rodgers, C., Rafidi, K., Zou, A., Xiao, J., Yan, S.(2011) Bioorg Med Chem Lett 21: 1270-1274
- PubMed: 21269826
- DOI: https://doi.org/10.1016/j.bmcl.2010.12.026
- Primary Citation of Related Structures:
3PRE, 3PRZ, 3PS6 - PubMed Abstract:
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.
Organizational Affiliation:
Pfizer Global Research and Development, Chemistry Department, 10770 Science Center Drive, La Jolla, CA 92120, USA. Kevin.K.Liu@pfizer.com
