title: Synthesis and biological evaluation of (±)-3-(2-(2-fluorobenzyloxy) naphthalen-6-yl)-2-aminopropanoic acid derivatives as novel PTP1B inhibitors.
abstract: A series of novel nonphosphonate-based pTyr mimetics comprised (±)-3-(2-(2-fluorobenzyloxy)naphthalen-6-yl)-2-aminopropanoic acid derivatives were identified as reversible and competitive PTP1B inhibitors via a structure-based design approach. Among the compounds studied, 12h was found to have the best in vitro inhibition activity against PTP1B (IC(50) = 1.25 ± 0.24 μM) and the best selectivity (3-fold) between PTP1B and TCPTP. These results should provide suitable druglike lead compounds for the design of inhibitors of PTP1B as well as other PTPs.
authors.affiliation: Key Laboratory of Natural Resources of Changbai Mountain & Functional Molecules, Ministry of Education, Yanbian University College of Pharmacy, Yanji 133000, PR China.
authors.forename: Liang-Peng
authors.initials: LP
authors.lastname: Sun
authors.forename: Qiang
authors.initials: Q
authors.lastname: Shen
authors.forename: Hong-Hua
authors.initials: HH
authors.lastname: Piao
authors.forename: Wei-Ping
authors.initials: WP
authors.lastname: Ma
authors.forename: Li-Xin
authors.initials: LX
authors.lastname: Gao
authors.forename: Wei
authors.initials: W
authors.lastname: Zhang
authors.forename: Fa-Jun
authors.initials: FJ
authors.lastname: Nan
authors.forename: Jia
authors.initials: J
authors.lastname: Li
authors.forename: Hu-Ri
authors.initials: HR
authors.lastname: Piao
mesh_terms: D004791:Enzyme Inhibitors / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D020128:Inhibitory Concentration 50; D009682:Magnetic Resonance Spectroscopy; D011422:Propionates / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D054562:Protein Tyrosine Phosphatase, Non-Receptor Type 1 / Q000037:antagonists & inhibitors*
chemical_list: D004791:Enzyme Inhibitors; D011422:Propionates; D054562:Protein Tyrosine Phosphatase, Non-Receptor Type 1