Paclitaxel is a naturally occurring antimitotic agent that has been shown to stabilize microtubules, induce mitotic arrest, and ultimately induce apoptotic cell death. The favorable clinical activity of paclitaxel has prompted considerable interest in combining paclitaxel with numerous other antineoplastic agents. Our previous studies have suggested 5-fluorouracil (5-FU), an antineoplastic agen...

Compound 8H is a phenylcinnamide that induces G2/M-phase cell cycle arrest and cell death in cancer cell lines. Here we show that 8H exerts its cytotoxic activity through disruption of microtubule dynamics in vitro and in cell culture. A series of cinnamide derivatives were synthesized and evaluated, and several new compounds were identified that improve on the activity of the parent compound, ...

Antimitotic agents have been the most successful pharmacological agents for the treatment of cancer. The term "antimitotic agent" has traditionally been synonymous with tubulin-targeting compounds, but as a consequence of the large number of new compounds and mechanisms that have been identified recently, a much broader definition is currently needed. This review attempts to provide a broad ove...

Several antimitotic, tubulin-binding agents, such as colchicine, colcemid, and podophyllotoxin, inhibit the capping of fluorescent-labeled concanavalin A in Chinese hamster ovary cells. By comparing the effects of these agents on parental cell lines on several independently selected colchicine-resistant mutants with decreased drug permeability, we have demonstrated that permeation of these drug...

The taccalonolides are novel antimitotic microtubule stabilizers that have a unique mechanism of action independent of a direct interaction with tubulin. Cytotoxicity and clonogenic assays show that taccalonolide A and radiation act in an additive manner to cause cell death. The taxanes and epothilones have utility when combined with radiotherapy and these findings further suggest the additive ...

We report a novel method for screening and quantifying tubulin-binding antimitotic agents that promote microtubule formation. The method is based on the shift in the peak of the fluorescence emission difference spectrum of tubulin complexed to metal free tetrakis(4-carboxyphenyl)porphyrin (TCPP) in the presence of antimitotic agents. Taxol (paclitaxel), an anti-tumor drug approved for the treat...

antitumor and antifungal agents. Recently, curacin A, which is a potential antitumor agent, was isolated from marine cyanobacterium (blue-green alga) Lyngbya majuscula as an antimitotic cytotoxic component.1} We have reported an effective assay method for antimitotic substances, which observes deformations of mycelia germinated from conidia of Pyricularia oryzae P-2b, and certain antimitotic co...