1083326-17-3Relevant articles and documents
Bioisosteric replacements of the indole moiety for the development of a potent and selective PI3Kδ inhibitor: Design, synthesis and biological evaluation
Chen, Yi,Chen, Zhenxia,Deng, Mingli,Hong, Hui,Jia, Yu,Li, Qingquan,Li, Zhipeng,Ling, Yun,Liu, Xiaofeng,Lu, Mingzhu,Wu, Tianze,Xu, Chenyue,Yang, Chengbin,Yang, Yongtai,Zhou, Yaming
supporting information, (2021/07/10)
Based on indole scaffold, a potent and selective phosphoinositide 3-kinase delta (PI3Kδ) inhibitor, namely FD223, was developed by the bioisosteric replacement drug discovery approach and studied for the treatment of acute myeloid leukemia (AML). In vitro
Discovery of cinnoline derivatives as potent PI3K inhibitors with antiproliferative activity
Chen, Yi,Deng, Mingli,Jia, Yu,Ling, Yun,Liu, Xiaofeng,Lu, Mingzhu,Tian, Chengze,Wu, Tianze,Yang, Chengbin,Yang, Yongtai,Zhou, Yaming
supporting information, (2021/07/28)
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 displ
Discovery of 6′-chloro-N-methyl-5’-(phenylsulfonamido)-[3,3′-bipyridine]-5-carboxamide (CHMFL-PI4K-127) as a novel Plasmodium falciparum PI(4)K inhibitor with potent antimalarial activity against both blood and liver stages of Plasmodium
Liang, Xiaofei,Jiang, Zongru,Huang, Zhenghui,Li, Feng,Chen, Cheng,Hu, Chen,Wang, Wenliang,Hu, Zhenquan,Liu, Qingwang,Wang, Beilei,Wang, Li,Qi, Ziping,Liu, Jing,Jiang, Lubin,Liu, Qingsong
, (2020/02/06)
Starting from a bipyridine-sulfonamide scaffold, medicinal chemistry optimization leads to the discovery of a novel Plasmodium falciparum PI4K kinase (PfPI4K) inhibitor compound 15g (CHMFL-PI4K-127, IC50: 0.9 nM), which exhibits potent activity against 3D7 Plasmodium falciparum (P. falciparum) (EC50: 25.1 nM). CHMFL-PI4K-127 displays high selectivity against PfPI4K over human lipid and protein kinase. In addition, it exhibits EC50 values of 23–47 nM against a panel of the drug-resistant strains of P. falciparum. In vivo, the inhibitor demonstrates the favorable pharmacokinetic properties in both rats and mice. Furthermore, oral administration of CHMFL-PI4K-127 exhibits the antimalaria efficacy in both blood stage (80 mg/kg) and liver stage (1 mg/kg) of Plasmodium in infected rodent model. The results suggest that CHMFL-PI4K-127 might be a new potential drug candidate for malaria.