title: Pyrazinoindolone inhibitors of MAPKAP-K2.
abstract: Optimization of pyrazinoindolone inhibitors of MAPKAP-K2 (MK2) provides a reasonable balance of cellular potency and physicochemical properties. Mechanistic studies support the inhibition of MK2 which is responsible for the sub-micromolar cellular efficacy.
authors.affiliation: Department of Medicinal Chemistry, Boehringer Ingelheim Pharmaceuticals, Inc., Research and Development Center, 900 Ridgebury Road, Ridgefield, CT 06877, USA. dgoldber@rdg.boehringer-ingelheim.com
authors.forename: D R
authors.initials: DR
authors.lastname: Goldberg
authors.forename: Y
authors.initials: Y
authors.lastname: Choi
authors.forename: D
authors.initials: D
authors.lastname: Cogan
authors.forename: M
authors.initials: M
authors.lastname: Corson
authors.forename: R
authors.initials: R
authors.lastname: DeLeon
authors.forename: A
authors.initials: A
authors.lastname: Gao
authors.forename: L
authors.initials: L
authors.lastname: Gruenbaum
authors.forename: M H
authors.initials: MH
authors.lastname: Hao
authors.forename: D
authors.initials: D
authors.lastname: Joseph
authors.forename: M A
authors.initials: MA
authors.lastname: Kashem
authors.forename: C
authors.initials: C
authors.lastname: Miller
authors.forename: N
authors.initials: N
authors.lastname: Moss
authors.forename: M R
authors.initials: MR
authors.lastname: Netherton
authors.forename: C P
authors.initials: CP
authors.lastname: Pargellis
authors.forename: J
authors.initials: J
authors.lastname: Pelletier
authors.forename: R
authors.initials: R
authors.lastname: Sellati
authors.forename: D
authors.initials: D
authors.lastname: Skow
authors.forename: C
authors.initials: C
authors.lastname: Torcellini
authors.forename: Y-C
authors.initials: YC
authors.lastname: Tseng
authors.forename: J
authors.initials: J
authors.lastname: Wang
authors.forename: R
authors.initials: R
authors.lastname: Wasti
authors.forename: B
authors.initials: B
authors.lastname: Werneburg
authors.forename: J P
authors.initials: JP
authors.lastname: Wu
authors.forename: Z
authors.initials: Z
authors.lastname: Xiong
mesh_terms: D020650:Combinatorial Chemistry Techniques; D004791:Enzyme Inhibitors / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D007211:Indoles / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D020128:Inhibitory Concentration 50; D047908:Intracellular Signaling Peptides and Proteins / Q000037:antagonists & inhibitors*; D015394:Molecular Structure; D017346:Protein Serine-Threonine Kinases / Q000037:antagonists & inhibitors*; D011720:Pyrazoles / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D013329:Structure-Activity Relationship; D000099190:MAP-Kinase-Activated Kinase 2
chemical_list: D004791:Enzyme Inhibitors; D007211:Indoles; D047908:Intracellular Signaling Peptides and Proteins; D017346:Protein Serine-Threonine Kinases; D011720:Pyrazoles; D000099190:MAP-Kinase-Activated Kinase 2