Synthesis and cytotoxic activity of 2-acyl-1H-indole-4,7-diones on human cancer cell lines

Synthesis and cytotoxic activity of a series of 2-acyl-1H-indole-4,7-diones on human cancer cell lines are described. Due to close structural relationship to 2-acylindoles, potent inhibitors of tubulin polymerization, the mode of action of these novel compounds has been investigated. Cytotoxicity, t...

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Bibliographic Details
Published in:European journal of medicinal chemistry 2005, Vol.40 (1), p.85-92
Main Authors: MAHBOOBI, Siavosh, SELLMER, Andreas, EICHHORN, Emerich, BECKERS, Thomas, FIEBIG, Heinz-Herbert, KELTER, Gerhard
Format: Article
Language:English
Subjects:
Animals
Antineoplastic agents
Antineoplastic Agents - chemical synthesis
Antineoplastic Agents - pharmacology
Biological and medical sciences
Breast Neoplasms - drug therapy
Breast Neoplasms - pathology
Carrier Proteins - genetics
Cattle
Cell Cycle
Cell Line, Tumor
Cell Proliferation - drug effects
Cyclin-Dependent Kinase Inhibitor p27
General aspects
Humans
Indoles - chemical synthesis
Indoles - pharmacology
Inhibitory Concentration 50
Intracellular Signaling Peptides and Proteins - genetics
Ketones - chemical synthesis
Ketones - pharmacology
Kidney Neoplasms - drug therapy
Kidney Neoplasms - pathology
Medical sciences
Pharmacology. Drug treatments
Structure-Activity Relationship
Tubulin - drug effects
Tubulin - metabolism
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Summary:Synthesis and cytotoxic activity of a series of 2-acyl-1H-indole-4,7-diones on human cancer cell lines are described. Due to close structural relationship to 2-acylindoles, potent inhibitors of tubulin polymerization, the mode of action of these novel compounds has been investigated. Cytotoxicity, the influence on tubulin polymerization, and cell cycle dependent cytotoxicity on colon carcinoma cells by investigation of RKO exo p27 versus RKO p27(kip1) cells are described. IC50 values of arrested versus proliferating cells differ only in a range of two to fourfold and therefore cellular targets, predominantly relevant for mitotic progression, are excluded. As shown by the significant difference in the IC90 values on different tumor cell lines, the investigated compounds seem to act selectively on mammary and renal cancer cells.
ISSN:0223-5234
1768-3254
DOI:10.1016/j.ejmech.2004.10.007