title: Discovery of di-indolinone as a novel scaffold for protein tyrosine phosphatase 1B inhibitors.
abstract: A series of di-indolinone derivatives was designed and synthesized to optimize our lead compounds basing on molecular docking study as PTP1B inhibitors. Successive enzymatic assay identified the synthetic di-indolinone as novel PTP1B inhibitors with low micromole-ranged inhibitory activity and at least several-fold selectivity over other tested homologous PTPs.
authors.affiliation: Shanghai Key Laboratory of New Drug Design, School of Pharmacy, East China University of Science and Technology, Shanghai 200237, PR China.
authors.forename: Hou-ling
authors.initials: HL
authors.lastname: Dai
authors.forename: Li-xin
authors.initials: LX
authors.lastname: Gao
authors.forename: Ying
authors.initials: Y
authors.lastname: Yang
authors.forename: Jing-ya
authors.initials: JY
authors.lastname: Li
authors.forename: Jia-gao
authors.initials: JG
authors.lastname: Cheng
authors.forename: Jia
authors.initials: J
authors.lastname: Li
authors.forename: Ren
authors.initials: R
authors.lastname: Wen
authors.forename: Yan-qing
authors.initials: YQ
authors.lastname: Peng
authors.forename: Jian-bin
authors.initials: JB
authors.lastname: Zheng
mesh_terms: D004305:Dose-Response Relationship, Drug; D055808:Drug Discovery; D004791:Enzyme Inhibitors / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D006801:Humans; D007211:Indoles / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D008958:Models, Molecular; D015394:Molecular Structure; D054562:Protein Tyrosine Phosphatase, Non-Receptor Type 1 / Q000037:antagonists & inhibitors* / Q000378:metabolism; D013329:Structure-Activity Relationship
chemical_list: D004791:Enzyme Inhibitors; D007211:Indoles; C516607:PTPN1 protein, human; D054562:Protein Tyrosine Phosphatase, Non-Receptor Type 1