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A minilibrary of cationic N-heterocycles has been prepared and evaluated. The potential for the preparation was a result of the high versatility of palladium-mediated chemistry. The synthesis of the novel molecules was based on intramolecular quaternization of tertiary amine attached allylpalladium complexes. The steric and electronic factors of the reaction are discussed. The structures of the synthesized molecules made them candidates for precise biological and pharmaco-

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Several aminomethylene analogs and a ketomethylene analog of reversins were synthesized in order to evaluate their ability to inhibit P-glycoprotein-mediated drug efflux in K562/R7 human leukemic cells overexpressing P-glycoprotein. These analogs retained good activity compared to cyclosporin A and the original reversins.