2. Academic Validation
  3. Discovery of cinnoline derivatives as potent PI3K inhibitors with antiproliferative activity

Discovery of cinnoline derivatives as potent PI3K inhibitors with antiproliferative activity

  • Bioorg Med Chem Lett. 2021 Sep 15;48:128271. doi: 10.1016/j.bmcl.2021.128271.
Chengze Tian 1,  Chengbin Yang 1,  Tianze Wu 1,  Mingzhu Lu 1,  Yi Chen 1,  Yongtai Yang 1,  Xiaofeng Liu 1,  Yun Ling 1,  Mingli Deng 1,  Yu Jia 2,  Yaming Zhou 3
Affiliations

Affiliations

  • 1 Shanghai Key Laboratory of Molecular Catalysis and Innovative Materials, Department of Chemistry, Fudan University, Shanghai, China.
  • 2 Shanghai Key Laboratory of Molecular Catalysis and Innovative Materials, Department of Chemistry, Fudan University, Shanghai, China. Electronic address: yujia@fudan.edu.cn.
  • 3 Shanghai Key Laboratory of Molecular Catalysis and Innovative Materials, Department of Chemistry, Fudan University, Shanghai, China. Electronic address: ymzhou@fudan.edu.cn.
PMID: 34284105 DOI: 10.1016/j.bmcl.2021.128271
Abstract

Cinnoline is a potential pharmacophore which has rarely been reported for uses as PI3K inhibitors. In this study, a series of cinnoline derivatives were developed as PI3K inhibitors and evaluated for enzymatic and cellular activities. Most compounds displayed nanomolar inhibitory activities against PI3Ks, among which 25 displayed high LLE and micromolar inhibitory potency against three human tumor cell lines (IC50 = 0.264 μM, 2.04 μM, 1.14 μM).

Keywords

Cinnoline; PI3K inhibitor; PI3K/Akt pathway.

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