In our probing of the structural features responsible for the inhibitory activity of aminoglutethimide [l, 344-aminophenyl)-3-ethylpiperidine-2, 6-dione] toward the cholesterol side-chain cleavage enzyme system desmolase and the estrogen-forming system aromatase, targets in the action of 1 against hormone-dependent mammary tumors, analogues in several categories have been synthesized and evaluated. Of the known ...