4,17β-dihydroxy-17α-picolyl-androsta-4,6-dien-3-one

4,17β-dihydroxy-17α-picolyl-androsta-4,6-dien-3-one is a synthetic steroidal derivative investigated for its potent antiproliferative and pro-apoptotic activities against breast cancer, including triple-negative breast cancer (TNBC) cell lines such as MDA-MB-231. Structurally, it combines a 4-hydroxy-androsta-4,6-diene-3-one scaffold with a 17α-picolyl (pyridin-2-ylmethyl) substituent. The compound induces cell death primarily through the activation of the apoptotic pathway, characterized by changes in cell cycle distribution and mitochondrial membrane potential. It was developed by researchers at the University of Novi Sad as part of a series of heterocyclic androstane derivatives aimed at overcoming resistance in receptor-negative breast cancers, which lack estrogen, progesterone, and HER2 receptors. While structurally related to aromatase and CYP17A1 inhibitors, its efficacy in TNBC suggests a direct cytotoxic mechanism through the induction of programmed cell death.

Other names

4,17β-dihydroxy-17α-(pyridin-2-ylmethyl)androsta-4,6-dien-3-one4,17β-dihydroxy-17α-picolyl-androsta-4,6-dien-3-one