Structure-activity relationship of N-methyl-bisindolylmaleimide derivatives as cell death inhibitors.
A series of N-methyl-bisindolylmaleimide derivatives was synthesized and evaluated as cell death inhibitors. N-Methyl-2-[1-(3-aminopropyl)-1H-indol-3-yl]-3-(1H-indol-3-yl)maleimide (21) was the most potent inhibitor of H2O2-induced necrotic death of human leukemia HL60 cells among them.
Katoh
Miho
M
Institute of Multidisciplinary Research for Advanced Materials (IMRAM), Tohoku University, 2-1-1 Katahira, Aoba, Sendai, Miyagi 980-8577, Japan.
Dodo
Kosuke
K
Fujita
Mikako
M
Sodeoka
Mikiko
M
D000970:Antineoplastic Agents / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D016923:Cell Death / Q000187:drug effects*; D004791:Enzyme Inhibitors / Q000494:pharmacology; D018922:HL-60 Cells / Q000187:drug effects / Q000473:pathology; D006801:Humans; D006861:Hydrogen Peroxide / Q000494:pharmacology; D007211:Indoles / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D008301:Maleimides / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D015394:Molecular Structure; D009336:Necrosis; D016877:Oxidants / Q000494:pharmacology; D011494:Protein Kinases / Q000737:chemistry; D013329:Structure-Activity Relationship
D000970:Antineoplastic Agents; D004791:Enzyme Inhibitors; D007211:Indoles; D008301:Maleimides; C503756:N-methyl-2-(1-(3-aminopropyl)-1H-indol-3-yl)-3-(1H-indol-3-yl)maleimide; D016877:Oxidants; D006861:Hydrogen Peroxide; D011494:Protein Kinases; C088060:bisindolylmaleimide