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Lin S.,are Pharmaceutical R and nter | Han F.,are Pharmaceutical R and nter | Liu P.,are Pharmaceutical R and nter | Tao J.,are Pharmaceutical R and nter | And 4 more authors.
Bioorganic and Medicinal Chemistry Letters | Year: 2014

Inhibition of the phosphoinositide 3-kinase (PI3K)/AKT/mammalian target of rapamycin (mTOR) signaling pathway is one of the most intensively studied approaches to cancer therapy. Rational design led to the identification of novel 7-amino-5-methyl-1,6-naphthyridin-2(1H)-one derivatives as potent PI3K/mTOR dual inhibitors. Design, synthesis and structure activity relationship are reported. © 2014 Elsevier Ltd. All rights reserved. Source


Han F.,are Pharmaceutical R and nter | Lin S.,are Pharmaceutical R and nter | Liu P.,are Pharmaceutical R and nter | Liu X.,are Pharmaceutical R and nter | And 4 more authors.
ACS Medicinal Chemistry Letters | Year: 2015

Inhibition of the phosphoinositide 3-kinase (PI3K)/AKT/mammalian target of rapamycin (mTOR) signaling pathway provides a promising new approach for cancer therapy. Through a rational design, a novel series of thienopyrimidine was discovered as highly potent and selective PI3K inhibitors. These thienopyrimidine derivatives were demonstrated to bear nanomolar PI3Kα inhibitory potency with over 100-fold selectivity against mTOR kinase. The lead compounds 6g and 6k showed good developability profiles in cell-based proliferation and ADME assays. In this communication, their design, synthesis, structure-activity relationship, selectivity, and some developability properties are described. © 2015 American Chemical Society. Source

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