title: Mixed lineage kinase activity of indolocarbazole analogues.
abstract: The MLK1-3 activity for a series of analogues of the indolocarbazole K-252a is reported. Addition of 3,9-bis-alkylthiomethyl groups to K-252a results in potent and selective MLK inhibitors. The in vitro and in vivo survival promoting activity of bis-isopropylthiomethyl-K-252a (16, CEP-11004/KT-8138) is reported.
authors.affiliation: Kyowa-Hakko Kogyo Co., Ltd., Tokyo, Japan.
authors.forename: Chikara
authors.initials: C
authors.lastname: Murakata
authors.forename: Masami
authors.initials: M
authors.lastname: Kaneko
authors.forename: George
authors.initials: G
authors.lastname: Gessner
authors.forename: Thelma S
authors.initials: TS
authors.lastname: Angeles
authors.forename: Mark A
authors.initials: MA
authors.lastname: Ator
authors.forename: Teresa M
authors.initials: TM
authors.lastname: O'Kane
authors.forename: Beth Ann W
authors.initials: BA
authors.lastname: McKenna
authors.forename: Beth Ann
authors.initials: BA
authors.lastname: Thomas
authors.forename: Joanne R
authors.initials: JR
authors.lastname: Mathiasen
authors.forename: Michael S
authors.initials: MS
authors.lastname: Saporito
authors.forename: Donna
authors.initials: D
authors.lastname: Bozyczko-Coyne
authors.forename: Robert L
authors.initials: RL
authors.lastname: Hudkins
mesh_terms: D000818:Animals; D002227:Carbazoles / Q000494:pharmacology*; D002460:Cell Line; D004791:Enzyme Inhibitors / Q000494:pharmacology*; D020930:MAP Kinase Kinase Kinases / Q000037:antagonists & inhibitors*; D051379:Mice
chemical_list: D002227:Carbazoles; D004791:Enzyme Inhibitors; C041514:carbazole; D020930:MAP Kinase Kinase Kinases