New cyclopentane derivatives as inhibitors of steroid metabolizing enzymes AKR1C1 and AKR1C3

A series of cyclopentane derivatives was synthesized and evaluated for inhibition of the steroid metabolizing enzymes AKR1C1 and AKR1C3. Selective inhibitors that are active in the low micromolar range were identified. These compounds represent promising starting points in the development of new anticancer agents for the treatment of hormone-dependent forms of cancer and other diseases where AKR1C1 and AKR1C3 are involved.

Graphical abstractA series of new inhibitors of the AKR1C1 and AKR1C3 based on cyclopentane scaffold are presented.Figure optionsDownload full-size imageDownload as PowerPoint slide