Sulfonate Derivatives of Naphtho[2,3-b]thiophen-4(9H)-one and 9(10H)-Anthracenone as Highly Active Antimicrotubule Agents. Synthesis, Antiproliferative Activity, and Inhibition of Tubulin Polymerization

Sulfonate Derivatives of Naphtho[2,3-b]thiophen-4(9H)-one and 9(10H)-Anthracenone as Highly Active Antimicrotubule Agents. Synthesis, Antiproliferative Activity, and Inhibition of Tubulin Polymerization

Benzenesulfonate derivatives of naphtho[2,3-b]thiophen-4(9H)-one and 9(10H)-anthracenone were prepared and found to inhibit microtubule formation by an in vitro tubulin polymerization assay. Several analogues showed potent cytotoxic activity in an assay based on K562 leukemia cells with IC50 values...

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Veröffentlicht in:Journal of medicinal chemistry 2007-11, Vol.50 (24), p.6059-6066
Hauptverfasser: Zuse, Anne, Schmidt, Peter, Baasner, Silke, Böhm, Konrad J, Müller, Klaus, Gerlach, Matthias, Günther, Eckhard G, Unger, Eberhard, Prinz, Helge
Format: Artikel
Sprache:eng
Schlagworte:
Anthracenes - chemical synthesis
Anthracenes - chemistry
Anthracenes - pharmacology
Antineoplastic agents
Biological and medical sciences
Cell Cycle - drug effects
Cell Line, Tumor
Colchicine - pharmacology
Drug Resistance, Neoplasm
Drug Screening Assays, Antitumor
General aspects
Humans
Medical sciences
Naphthalenes - chemical synthesis
Naphthalenes - chemistry
Naphthalenes - pharmacology
Nocodazole - pharmacology
Pharmacology. Drug treatments
Podophyllotoxin - pharmacology
Structure-Activity Relationship
Thiophenes - chemical synthesis
Thiophenes - chemistry
Thiophenes - pharmacology
Tubulin - chemistry
Tubulin - metabolism
Tubulin Modulators - chemical synthesis
Tubulin Modulators - chemistry
Tubulin Modulators - pharmacology
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Zusammenfassung:Benzenesulfonate derivatives of naphtho[2,3-b]thiophen-4(9H)-one and 9(10H)-anthracenone were prepared and found to inhibit microtubule formation by an in vitro tubulin polymerization assay. Several analogues showed potent cytotoxic activity in an assay based on K562 leukemia cells with IC50 values of
ISSN:0022-2623
1520-4804
DOI:10.1021/jm0708984