A new class of phosphoinositide-dependent kinase-1 (PDK-1) inhibitors offormula (I): wherein X is selected from the group consisting of alkyl andhaloalkyl； Ar is an aryl radical selected from the group consisting of phenyl,biphenyl, naphthyl, anthryl, phenanthryl, and fluorenyl； and wherein Ar isoptionally substituted with one or more radicals selected from the groupconsisting of halo, C1 C4 alkyl, C1 C4 haloalkyl, azido, C1 C4 azidoalkyl,aryl, akylaryl, haloaryl, haloalkylaryl, and combinations thereof； and R isselected from the group consisting of nitrile, acetonitrile, ethylnitrile,propylnitrile, carboxamide, amidine, tetrazole, oxime, hydrazone, acetamidine,aminoacetamide, guanidine, and urea. Also provided are methods of using thecompounds for the treatment and prevention of cancer in humans.
