Hongping Jiang, Xirong Liu, Chunling Zeng, Jie Tang, Guofang Jiang
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引用次数: 0
Abstract
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 11d and 11f, which possess 3-acetyl and 17-pyridine (or 17-benzimidazole) moieties, exhibit enhanced cytotoxicity against DU145 and HCT116 cells.
期刊介绍：
Journal of Organic Chemistry welcomes original contributions of fundamental research in all branches of the theory and practice of organic chemistry. In selecting manuscripts for publication, the editors place emphasis on the quality and novelty of the work, as well as the breadth of interest to the organic chemistry community.
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