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- W798453310 abstract "Proc Amer Assoc Cancer Res, Volume 45, 20045439 A long term goal of our work is the identification of new microtubule disrupting agents that might have utility in the treatment of cancer. Microtubule stabilizers and microtubule depolymerizers have proved to be useful anticancer agents. Although our previous efforts focused mainly on identifying microtubule disrupting compounds from natural products, we recently began screening large synthetic chemical libraries to identify small molecule inhibitors of microtubules. A novel microtubule-depolymerizing compound with a molecular weight of 365 was identified using the phenotypic screening assay. The compound, designated CB694, is a potent inhibitor of cellular proliferation with an average IC50 value of 85 nM against a wide range of cancer cell lines. The NCI/ADR cell line, which has a high level of expression of P-glycoprotein, is resistant to the vinca alkaloids and Taxol and yet it is very sensitive to inhibition by CB694, suggesting that this compound is a poor substrate for transport by P-glycoprotein. Similar to the effects of the vinca alkaloids, CB694 causes loss of interphase microtubules. The lowest concentrations of CB694 cause loss of the microtubules at the cell periphery and higher concentrations cause complete depletion of cellular microtubules. Similar to the effects of other microtubule disrupting compounds, CB694 causes micronucleation and the formation of abnormal mitotic spindles. A concentration dependent increase in multipolar mitotic spindles occurs in HeLa cells treated with this compound. As expected from the effects on mitotic spindles, CB694 causes mitotic accumulation followed by G1 aneuploidy and apoptosis. The compound was also evaluated for efficacy against a syngeneic, transplantable solid tumor model. CB694, given on a qDx6 intravenous treatment schedule, was well tolerated and produced antitumor activity against early stage Mammary Adenocarcinoma 16/C. Supported by a grant from the William Randolph Hearst Foundation to SLM." @default.
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- W798453310 date "2004-04-01" @default.
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- W798453310 title "Identification of a novel synthetic microtubule depolymerizer with antitumor activity" @default.
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