title: Synthesis of novel 3-aryl-1-oxa-2,8-diazaspiro[4.5]dec-2-ene derivatives and their biological evaluation against protein tyrosine phosphatase 1B.
abstract: A series of novel 3-aryl-1-oxa-2,8-diazaspiro[4.5]dec-2-ene derivatives were designed, synthesized, and evaluated as a new class of inhibitors against protein tyrosine phosphatase 1B. Among them, compound 6f displayed moderate inhibitory activity with IC50 of 2.87 ± 0.24 μm and can be used as a novel lead compound for the design of inhibitors of protein tyrosine phosphatase 1B.
authors.affiliation: School of Pharmaceutical Science, Jiangnan University, Wuxi, 214122, China.|State key Laboratory of Drug Research, National Center for Drug Screening, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Shanghai, 201203, China.
authors.forename: Wen-Long
authors.initials: WL
authors.lastname: Wang
authors.affiliation: School of Pharmaceutical Science, Jiangnan University, Wuxi, 214122, China.
authors.forename: Xia
authors.initials: X
authors.lastname: Chen
authors.affiliation: State key Laboratory of Drug Research, National Center for Drug Screening, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Shanghai, 201203, China.
authors.forename: Li-Xin
authors.initials: LX
authors.lastname: Gao
authors.affiliation: State key Laboratory of Drug Research, National Center for Drug Screening, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Shanghai, 201203, China.
authors.forename: Li
authors.initials: L
authors.lastname: Sheng
authors.affiliation: State key Laboratory of Drug Research, National Center for Drug Screening, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Shanghai, 201203, China.
authors.forename: Jing-Ya
authors.initials: JY
authors.lastname: Li
authors.affiliation: State key Laboratory of Drug Research, National Center for Drug Screening, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Shanghai, 201203, China.
authors.forename: Jia
authors.initials: J
authors.lastname: Li
authors.affiliation: School of Pharmaceutical Science, Jiangnan University, Wuxi, 214122, China.
authors.forename: Bainian
authors.initials: B
authors.lastname: Feng
mesh_terms: D015195:Drug Design; D004791:Enzyme Inhibitors / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D006801:Humans; D054562:Protein Tyrosine Phosphatase, Non-Receptor Type 1 / Q000037:antagonists & inhibitors* / Q000378:metabolism; D013141:Spiro Compounds / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D013329:Structure-Activity Relationship
chemical_list: D004791:Enzyme Inhibitors; D013141:Spiro Compounds; C516607:PTPN1 protein, human; D054562:Protein Tyrosine Phosphatase, Non-Receptor Type 1
keywords: 3-aryl-1-oxa-2,8-diazaspiro[4.5]dec-2-ene derivatives; inhibitors; one-pot synthesis; protein tyrosine phosphatase 1B; structure-activity relationships