A small library of novel 1,3-oxazole sulfonamides were synthesized and evaluated for their ability to affect cancer cell growth. All compounds prepared were screened against the full NCI-60 human tumor cell panel and many possessed promising overall growth inhibitory properties. Of the cell lines tested, leukemia sub-panels were observed to be particularly sensitive to the library, with GI50 values falling within the low micromolar to nanomolar ranges. Compounds featuring a halogenated aniline moiety were exceptionally active, with most examples inhibiting cancer cell growth by at least 75%. Preliminary mode of action studies suggest that these compounds bind to tubulin and induce depolymerization of microtubules within cells.

Synthesis and antiproliferative activity of novel 1,3-oxazole sulfonamides

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