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  • Title: Potent antitubulin tumor cell cytotoxins based on 3-aroyl indazoles.
    Author: Duan JX, Cai X, Meng F, Lan L, Hart C, Matteucci M.
    Journal: J Med Chem; 2007 Mar 08; 50(5):1001-6. PubMed ID: 17286393.
    Abstract:
    A series of 3-aroyl indazoles was synthesized. Modification of the C-7 position resulted in a significant structure-activity relationship (SAR) with acetylene modifications conferring unusual potency in a tumor cell cytotoxicity assay. The most potent compounds exceeded the activity of combretastatin A4 (CA-4), showing single digit nM IC50 values against all cell lines tested including those with known efflux resistance pumps. The inhibition of in vitro tubulin polymerization was comparable to CA-4, consistent with tubulin being the target for these compounds. Competition binding experiments employing [3H]colchicine and purified tubulins demonstrated that the compound specifically binds to the colchicine site.
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