Structure-activity relationship of N-methyl-bisindolylmaleimide derivatives as cell death inhibitors

Miho Katoh; Kosuke Dodo; Mikako Fujita; Mikiko Sodeoka

doi:10.1016/j.bmcl.2005.04.015

Structure-activity relationship of N-methyl-bisindolylmaleimide derivatives as cell death inhibitors

Bioorg Med Chem Lett. 2005 Jun 15;15(12):3109-13. doi: 10.1016/j.bmcl.2005.04.015.

Authors

Miho Katoh¹, Kosuke Dodo, Mikako Fujita, Mikiko Sodeoka

Affiliation

¹ Institute of Multidisciplinary Research for Advanced Materials (IMRAM), Tohoku University, 2-1-1 Katahira, Aoba, Sendai, Miyagi 980-8577, Japan.

PMID: 15896957
DOI: 10.1016/j.bmcl.2005.04.015

Abstract

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.

Publication types

Comparative Study
Research Support, Non-U.S. Gov't

MeSH terms

Antineoplastic Agents / chemical synthesis
Antineoplastic Agents / chemistry*
Antineoplastic Agents / pharmacology*
Cell Death / drug effects*
Enzyme Inhibitors / pharmacology
HL-60 Cells / drug effects
HL-60 Cells / pathology
Humans
Hydrogen Peroxide / pharmacology
Indoles / chemical synthesis
Indoles / chemistry*
Indoles / pharmacology*
Maleimides / chemical synthesis
Maleimides / chemistry*
Maleimides / pharmacology*
Molecular Structure
Necrosis
Oxidants / pharmacology
Protein Kinases / chemistry
Structure-Activity Relationship

Substances

Antineoplastic Agents
Enzyme Inhibitors
Indoles
Maleimides
N-methyl-2-(1-(3-aminopropyl)-1H-indol-3-yl)-3-(1H-indol-3-yl)maleimide
Oxidants
Hydrogen Peroxide
Protein Kinases
bisindolylmaleimide