Structural highlights
Publication Abstract from PubMed
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 PI3Kgamma enzyme. In addition, a novel synthetic route was developed for these analogs.
Quinazolines with intra-molecular hydrogen bonding scaffold (iMHBS) as PI3K/mTOR dual inhibitors.,Liu KK, Huang X, Bagrodia S, Chen JH, Greasley S, Cheng H, Sun S, Knighton D, Rodgers C, Rafidi K, Zou A, Xiao J, Yan S Bioorg Med Chem Lett. 2011 Feb 15;21(4):1270-4. Epub 2010 Dec 10. PMID:21269826[1]
From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.
See Also
References
- ↑ Liu KK, Huang X, Bagrodia S, Chen JH, Greasley S, Cheng H, Sun S, Knighton D, Rodgers C, Rafidi K, Zou A, Xiao J, Yan S. Quinazolines with intra-molecular hydrogen bonding scaffold (iMHBS) as PI3K/mTOR dual inhibitors. Bioorg Med Chem Lett. 2011 Feb 15;21(4):1270-4. Epub 2010 Dec 10. PMID:21269826 doi:10.1016/j.bmcl.2010.12.026
