title: Synthesis and SAR of novel imidazoquinoxaline-based Lck inhibitors: improvement of cell potency.
abstract: A series of anilino(imidazoquinoxaline) analogues bearing solubilizing side chains at the 6- and 7-positions of the fused phenyl ring has been prepared and evaluated for inhibition against Lck enzyme and of T-cell proliferation. Significant improvement of the cellular activity was achieved over the initial lead, compound 2.
authors.affiliation: Discovery Chemistry, Bristol Myers Squibb Pharmaceutical Research Institute, PO Box 4000, Princeton, NJ 08543, USA. ping.chen@bms.com
authors.forename: Ping
authors.initials: P
authors.lastname: Chen
authors.forename: Edwin J
authors.initials: EJ
authors.lastname: Iwanowicz
authors.forename: Derek
authors.initials: D
authors.lastname: Norris
authors.forename: Henry H
authors.initials: HH
authors.lastname: Gu
authors.forename: James
authors.initials: J
authors.lastname: Lin
authors.forename: Robert V
authors.initials: RV
authors.lastname: Moquin
authors.forename: Jagabandhu
authors.initials: J
authors.lastname: Das
authors.forename: John
authors.initials: J
authors.lastname: Wityak
authors.forename: Steven H
authors.initials: SH
authors.lastname: Spergel
authors.forename: Henry
authors.initials: H
authors.lastname: de Fex
authors.forename: Suhong
authors.initials: S
authors.lastname: Pang
authors.forename: Sydney
authors.initials: S
authors.lastname: Pitt
authors.forename: Ding Ren
authors.initials: DR
authors.lastname: Shen
authors.forename: Gary L
authors.initials: GL
authors.lastname: Schieven
authors.forename: Joel C
authors.initials: JC
authors.lastname: Barrish
mesh_terms: D002455:Cell Division / Q000187:drug effects; D004791:Enzyme Inhibitors / Q000138:chemical synthesis* / Q000494:pharmacology*; D006801:Humans; D007202:Indicators and Reagents; D019860:Lymphocyte Specific Protein Tyrosine Kinase p56(lck) / Q000037:antagonists & inhibitors*; D011810:Quinoxalines / Q000138:chemical synthesis* / Q000494:pharmacology*; D013329:Structure-Activity Relationship; D013601:T-Lymphocytes / Q000187:drug effects
chemical_list: D004791:Enzyme Inhibitors; D007202:Indicators and Reagents; D011810:Quinoxalines; D019860:Lymphocyte Specific Protein Tyrosine Kinase p56(lck)