e.g. Filippa Pettersson or Cancer Res. 75(6) , 1102-12, (2015) or 10.1002/anie.201600521
Analogs of 3-ethyl-3-(4-pyridyl) piperidine-2, 6-dione as selective inhibitors of aromatase: derivatives with variable 1-alkyl and 3-alkyl substituents
3-Ethyl-3-(4-pyridyl) piperidine-2, 6-dione (1) is a strong competitive inhibitor of human placental aromatase (Ki= 1.1 pM; testosterone as substrate) that, unlike the structurally related aromatase inhibitor aminoglutethimide (2), is not also an inhibitor of the cholesterol side-chain cleavage enzyme desmolase. An improved synthesis of 1 is described, which was readily adapted to the preparation of homologues in a series of 3-alkyl-3-(4-pyridyl)- ...
