Synthesis and structure-activity relationships of PI3K/mTOR dual inhibitors from a series of 2-amino-4-methylpyrido[2,3-d]pyrimidine derivatives

  • Bioorg Med Chem Lett. 2014 Sep 15;24(18):4538-4541. doi: 10.1016/j.bmcl.2014.07.073.
Fangbin Han  1 ,  Songwen Lin  1 ,  Peng Liu  1 ,  Jing Tao  1 ,  Chongqin Yi  1 ,  Heng Xu  2
Affiliations
  • 1. PKUCare Pharmaceutical R&D Center, A106-109, Biotech Innovation Works, No.29 Life Science Park Road, Changping District, Beijing 102206, PR China.
  • 2. PKUCare Pharmaceutical R&D Center, A106-109, Biotech Innovation Works, No.29 Life Science Park Road, Changping District, Beijing 102206, PR China. Electronic address: [email protected].
PMID: 25139570 DOI: 10.1016/j.bmcl.2014.07.073
Abstract

Inhibition of the phosphoinositide 3-kinase (PI3K)/Akt/mammalian target of rapamycin (mTOR) signaling pathway by PI3K/mTOR dual inhibitors provides a promising new approach to the treatment of cancers. In this Letter, we identified structurally novel and potent PI3K/mTOR dual inhibitors from a series of 2-amino-4-methylpyrido[2,3-d]pyrimidine derivatives. Their synthesis and structure-activity relationships are reported.

Keywords
Anti-tumor activity; Dual inhibitor; Mammalian target of rapamycin; Phosphoinositide 3-kinase.