title: Pyrrolo[2,3-c]azepine derivatives: a new class of potent protein tyrosine phosphatase 1B inhibitors.
abstract: A series of pyrrolo[2,3-c]azepine derivatives was designed, synthesized, and evaluated as a new class of inhibitors against protein tyrosine phosphatase 1B (PTP1B) in vitro. The results demonstrated that compounds bearing a biphenyl moiety were proved to markedly influence the potency of these inhibitors. Particularly, compounds 29, 35 and 36 showed interesting inhibition with IC(50) value of 16.36, 14.93 and 13.92μM, respectively.
authors.affiliation: School of Chemistry and Chemical Engineering, Sun Yat-Sen University, 135 West Xin Gang Road, Guangzhou 510275, China.
authors.forename: Jianwei
authors.initials: J
authors.lastname: Xie
authors.forename: Jinying
authors.initials: J
authors.lastname: Tian
authors.forename: Li
authors.initials: L
authors.lastname: Su
authors.forename: Manna
authors.initials: M
authors.lastname: Huang
authors.forename: Xinhai
authors.initials: X
authors.lastname: Zhu
authors.forename: Fei
authors.initials: F
authors.lastname: Ye
authors.forename: Yiqian
authors.initials: Y
authors.lastname: Wan
mesh_terms: D001381:Azepines / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology; D001713:Biphenyl Compounds / Q000737:chemistry; D004791:Enzyme Inhibitors / Q000737:chemistry* / Q000494:pharmacology; D006801:Humans; D007211:Indoles / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology; D054562:Protein Tyrosine Phosphatase, Non-Receptor Type 1 / Q000037:antagonists & inhibitors* / Q000235:genetics / Q000378:metabolism; D011758:Pyrroles / Q000737:chemistry*; D011994:Recombinant Proteins / Q000037:antagonists & inhibitors / Q000235:genetics / Q000378:metabolism; D013329:Structure-Activity Relationship
chemical_list: D001381:Azepines; D001713:Biphenyl Compounds; D004791:Enzyme Inhibitors; D007211:Indoles; D054562:Protein Tyrosine Phosphatase, Non-Receptor Type 1; D011758:Pyrroles; D011994:Recombinant Proteins; C010574:biphenyl