Mixed lineage kinase activity of indolocarbazole analogues.
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.
Murakata
Chikara
C
Kyowa-Hakko Kogyo Co., Ltd., Tokyo, Japan.
Kaneko
Masami
M
Gessner
George
G
Angeles
Thelma S
TS
Ator
Mark A
MA
O'Kane
Teresa M
TM
McKenna
Beth Ann W
BA
Thomas
Beth Ann
BA
Mathiasen
Joanne R
JR
Saporito
Michael S
MS
Bozyczko-Coyne
Donna
D
Hudkins
Robert L
RL
D000818:Animals; D002227:Carbazoles / Q000494:pharmacology*; D002460:Cell Line; D004791:Enzyme Inhibitors / Q000494:pharmacology*; D020930:MAP Kinase Kinase Kinases / Q000037:antagonists & inhibitors*; D051379:Mice
D002227:Carbazoles; D004791:Enzyme Inhibitors; C041514:carbazole; D020930:MAP Kinase Kinase Kinases