2. Academic Validation
  3. Discovery of a series of N-(5-(quinolin-6-yl)pyridin-3-yl)benzenesulfonamides as PI3K/mTOR dual inhibitors

Discovery of a series of N-(5-(quinolin-6-yl)pyridin-3-yl)benzenesulfonamides as PI3K/mTOR dual inhibitors

  • Eur J Med Chem. 2017 Feb 15:127:509-520. doi: 10.1016/j.ejmech.2017.01.016.
Jiankang Zhang 1,  Xiaoqing Lv 2,  Xiaodong Ma 3,  Yongzhou Hu 4
Affiliations

Affiliations

  • 1 Department of Pharmaceutical Preparation, Hangzhou Xixi Hospital, Hangzhou 310023, China.
  • 2 College of Medicine, Jiaxing University, Jiaxing 314001, China. Electronic address: lxqd1@126.com.
  • 3 Department of Medicinal Chemistry, School of Pharmacy, Anhui University of Chinese Medicine, Hefei 230031, China.
  • 4 College of Pharmaceutical Sciences, Zhejiang University, Hangzhou 310058, China.
PMID: 28109945 DOI: 10.1016/j.ejmech.2017.01.016
Abstract

Recently, the phosphoinositide 3-kinase (PI3K) and mammalian target of rapamycin (mTOR) have been considered as promising targets for the treatment of Cancer. Herein, we synthesized a series of N-(5-(quinolin-6-yl)pyridin-3-yl)benzenesulfonamides as novel PI3K/mTOR dual inhibitors for Cancer therapy. In the biological evaluation, compound 17e was identified as a potent PI3K/mTOR dual inhibitor, which significantly inhibit Class I PI3Ks, mTOR and phosphorylation of pAkt(Ser473) at low nanomolar level. Moreover, 17e display high potency against PC-3 cells (IC50 = 80 nM) in the anti-proliferative assay, and showed acceptable pharmacokinetic properties in vivo.

Keywords

Cancer; Inhibitor; PI3K; mTOR.

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