Isobenzofuran analogs of sclerophytin A are prepared in a highly concise fashion via an aldol-cycloaldol sequence. The analogs exhibit IC50s as low as 1 μM in growth inhibitory studies against KB3 cells using an MTT assay. Preferred analogs have one of the following structural formulas, where R is hydrogen or a substituted or unsubstituted lower alkyl group and Ar is a substituted or unsubstituted aryl group.
