A thalidomide analogue with in vitro antiproliferative, antimitotic, and microtubule-stabilizing activities

We discovered a thalidomide analogue [5-hydroxy-(2,6-diisopropylphenyl)-1H-isoindole-1,3-dione (5HPP-33)] with antiproliferative activity against nine cancer cell lines in vitro . Flow cytometric analyses showed that the compound caused G 2 -M arrest, which occurred mainly at the mitotic phase. In a...

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Veröffentlicht in:Molecular cancer therapeutics 2006-02, Vol.5 (2), p.450-456
Hauptverfasser: Li, Pui-Kai, Pandit, Bulbul, Sackett, Dan L, Hu, Zhigen, Zink, Jennifer, Zhi, Jiandong, Freeman, Dena, Robey, Robert W, Werbovetz, Karl, Lewis, Andrew, Li, Chenglong
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container_end_page 456
container_issue 2
container_start_page 450
container_title Molecular cancer therapeutics
container_volume 5
creator Li, Pui-Kai
Pandit, Bulbul
Sackett, Dan L
Hu, Zhigen
Zink, Jennifer
Zhi, Jiandong
Freeman, Dena
Robey, Robert W
Werbovetz, Karl
Lewis, Andrew
Li, Chenglong
description We discovered a thalidomide analogue [5-hydroxy-(2,6-diisopropylphenyl)-1H-isoindole-1,3-dione (5HPP-33)] with antiproliferative activity against nine cancer cell lines in vitro . Flow cytometric analyses showed that the compound caused G 2 -M arrest, which occurred mainly at the mitotic phase. In addition, immunofluorescence microscopy and in vitro tubulin polymerization studies showed that 5HPP-33 has antimicrotubule activity with a paclitaxel-like mode of action. It is effective against four different paclitaxel-resistant cell lines. Thus, 5HPP-33 represents a potential antitumor agent. [Mol Cancer Ther 2006;5(2):450–6]
doi_str_mv 10.1158/1535-7163.MCT-05-0254
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source MEDLINE; American Association for Cancer Research; EZB-FREE-00999 freely available EZB journals
subjects Animals
antimicrotubule
Antimitotic Agents - chemical synthesis
Antimitotic Agents - chemistry
Antimitotic Agents - pharmacology
Antineoplastic Agents - chemical synthesis
Antineoplastic Agents - chemistry
Antineoplastic Agents - pharmacology
Cell Cycle - drug effects
Cell Line, Tumor
Drug Resistance, Neoplasm
Humans
Indoles - chemical synthesis
Indoles - chemistry
Indoles - pharmacology
Isoindoles
Mice
multidrug resistance
Paclitaxel - pharmacology
thalidomide
tubulin
Tubulin - drug effects
Tubulin Modulators - chemical synthesis
Tubulin Modulators - chemistry
Tubulin Modulators - pharmacology
title A thalidomide analogue with in vitro antiproliferative, antimitotic, and microtubule-stabilizing activities
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