Enhanced Cytotoxicity of 10α,9β-Abiraterone Analogues Synthesized via LED Photocatalysis

Abiraterone and its analogues have been widely used in the treatment of castration-resistant prostate cancer (CRPC). However, these drugs suffer from limited bioavailability and pharmacological activity. Consequently, the modification of the abiraterone structure has become increasingly important and has attracted significant attention in recent years. This document presents 10-CH₃ transposable abiraterone analogues that can be synthesized through a series of 9 to 10 reaction steps, including an LED-induced photochemical conversion step to produce 10-CH₃-flipped compounds with high yields. Subsequently, the newly synthesized 10-CH₃ transposable compounds were evaluated in cytotoxicity assays, demonstrating that compounds <b>11d</b> and <b>11f</b>, which possess 3-acetyl and 17-pyridine (or 17-benzimidazole) moieties, exhibit enhanced cytotoxicity against DU145 and HCT116 cells.