Abstract:
:The identification and lead optimization of a series of pyridopyrimidinone derivatives are described as a novel class of efficacious dual PI3K/mTOR inhibitors, resulting in the discovery of 31. Compound 31 exhibited high enzyme activity against PI3K and mTOR, potent suppression of Akt and p70s6k phosphorylation in cell assays, and good pharmacokinetic profile. Furthermore, compound 31 demonstrated in vivo efficacy in a PC-3M tumor xenograft model.
journal_name
ACS Med Chem Lettjournal_title
ACS medicinal chemistry lettersauthors
Yu T,Li N,Wu C,Guan A,Li Y,Peng Z,He M,Li J,Gong Z,Huang L,Gao B,Hao D,Sun J,Pan Y,Shen L,Chan C,Lu X,Yuan H,Li Y,Li J,Chen Sdoi
10.1021/acsmedchemlett.8b00002subject
Has Abstractpub_date
2018-02-27 00:00:00pages
256-261issue
3issn
1948-5875journal_volume
9pub_type
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