title: 1H-2,3-dihydroperimidine derivatives: a new class of potent protein tyrosine phosphatase 1B inhibitors.
abstract: A series of 1H-2,3-dihydroperimidine derivatives was designed, synthesized, and evaluated as a new class of inhibitors of protein tyrosine phosphatase 1B (PTP1B) with IC50 values in the micromolar range. Compounds 46 and 49 showed submicromolar inhibitory activity against PTP1B, and good selectivity (3.48-fold and 2.10-fold respectively) over T-cell protein tyrosine phosphatases (TCPTP). These results have provided novel lead compounds for the design of inhibitors of PTP1B as well as other PTPs.
authors.affiliation: School of Pharmaceutical Science, Jiangnan University, Wuxi 214122, China. wwenlong2011@163.com.
authors.forename: Wen-Long
authors.initials: WL
authors.lastname: Wang
authors.forename: Dong-Lin
authors.initials: DL
authors.lastname: Yang
authors.forename: Li-Xin
authors.initials: LX
authors.lastname: Gao
authors.forename: Chun-Lan
authors.initials: CL
authors.lastname: Tang
authors.forename: Wei-Ping
authors.initials: WP
authors.lastname: Ma
authors.forename: Hui-Hua
authors.initials: HH
authors.lastname: Ye
authors.forename: Si-Qi
authors.initials: SQ
authors.lastname: Zhang
authors.forename: Ya-Nan
authors.initials: YN
authors.lastname: Zhao
authors.forename: Hao-Jie
authors.initials: HJ
authors.lastname: Xu
authors.forename: Zhao
authors.initials: Z
authors.lastname: Hu
authors.forename: Xia
authors.initials: X
authors.lastname: Chen
authors.forename: Wen-Hua
authors.initials: WH
authors.lastname: Fan
authors.forename: Hai-Jun
authors.initials: HJ
authors.lastname: Chen
authors.forename: Jing-Ya
authors.initials: JY
authors.lastname: Li
authors.forename: Fa-Jun
authors.initials: FJ
authors.lastname: Nan
authors.affiliation: School of Pharmaceutical Science, Jiangnan University, Wuxi 214122, China. jli@mail.shcnc.ac.cn.
authors.forename: Jia
authors.initials: J
authors.lastname: Li
authors.affiliation: School of Pharmaceutical Science, Jiangnan University, Wuxi 214122, China. fanwenhua1987@163.com.
authors.forename: Bainian
authors.initials: B
authors.lastname: Feng
mesh_terms: D000818:Animals; D016466:CHO Cells; D003412:Cricetulus; D020128:Inhibitory Concentration 50; D007700:Kinetics; D015394:Molecular Structure; D054562:Protein Tyrosine Phosphatase, Non-Receptor Type 1 / Q000037:antagonists & inhibitors*; D011799:Quinazolines / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D013329:Structure-Activity Relationship
chemical_list: D011799:Quinazolines; C022049:perimidine; D054562:Protein Tyrosine Phosphatase, Non-Receptor Type 1