An unhydrolyzable analogue of N-(4-hydroxyphenyl)retinamide: synthesis and preliminary biological studies

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• 作者：Weiss ; Kevin L. ; Alshafie ; Galal ; Chapman ; Jason S. ; Mershon ; Serena M. ; Abou-Issa ; Hussein ; et. al.
• 刊名：Bioorganic and Medicinal Chemistry Letters
• 出版年：2001
• 出版时间：June 18, 2001
• 年：2001
• 卷：11
• 期：12
• 页码：1583-1586
• 全文大小：175 K

文摘

The synthesis of a nonhydrolyzable, carbon-linked analogue (4-HBR) of the retinoid N-(4-hydroxyphenyl)retinamide (4-HPR) using Umpolung methods is described. Preliminary studies of biological activity show 4-HBR is similar to 4-HPR in its actions although a potentially relevant and desirable difference is its reduced suppression of plasma vitamin A levels. These results show that 4-HPR does not have to be hydrolyzed to retinoic acid to produce its chemotherapeutic effects.