title: PTP-1B inhibitors: cyclopenta[d][1,2]-oxazine derivatives.
abstract: A series of novel cyclopenta[d][1,2]-oxazine derivatives was prepared and evaluated for their inhibitory activity toward protein tyrosine phosphatase 1B (PTP-1B). Compound 6s was found to be an inhibitor of PTP-1B with nanomolar IC(50) value and high level of selectivity over other recombinant phosphatases.
authors.affiliation: Bio-Organic Science Division, Korea Research Institute of Chemical Technology, 100 Jang-dong, Yuseong-gu, Daejeon 305-600, Republic of Korea.
authors.forename: Sung Yun
authors.initials: SY
authors.lastname: Cho
authors.forename: Ji Yoen
authors.initials: JY
authors.lastname: Baek
authors.forename: Sang Sub
authors.initials: SS
authors.lastname: Han
authors.forename: Seung Kyu
authors.initials: SK
authors.lastname: Kang
authors.forename: Jae Du
authors.initials: JD
authors.lastname: Ha
authors.forename: Jin Hee
authors.initials: JH
authors.lastname: Ahn
authors.forename: Jae Don
authors.initials: JD
authors.lastname: Lee
authors.forename: Kwang Rok
authors.initials: KR
authors.lastname: Kim
authors.forename: Hyae Gyeong
authors.initials: HG
authors.lastname: Cheon
authors.forename: Sang Dal
authors.initials: SD
authors.lastname: Rhee
authors.forename: Sung Don
authors.initials: SD
authors.lastname: Yang
authors.forename: Gyu Hwan
authors.initials: GH
authors.lastname: Yon
authors.forename: Chwang Siek
authors.initials: CS
authors.lastname: Pak
authors.forename: Joong-Kwon
authors.initials: JK
authors.lastname: Choi
mesh_terms: D003517:Cyclopentanes / Q000138:chemical synthesis*; D015195:Drug Design; D004791:Enzyme Inhibitors / Q000138:chemical synthesis* / Q000494:pharmacology; D006801:Humans; D020128:Inhibitory Concentration 50; D010078:Oxazines / Q000138:chemical synthesis*; D054562:Protein Tyrosine Phosphatase, Non-Receptor Type 1; D017027:Protein Tyrosine Phosphatases / Q000037:antagonists & inhibitors*; D013329:Structure-Activity Relationship; D013379:Substrate Specificity
chemical_list: D003517:Cyclopentanes; D004791:Enzyme Inhibitors; D010078:Oxazines; C516607:PTPN1 protein, human; D054562:Protein Tyrosine Phosphatase, Non-Receptor Type 1; D017027:Protein Tyrosine Phosphatases