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

Autor: K L, Weiss, G, Alshafie, J S, Chapman, S M, Mershon, H, Abou-Issa, M, Clagett-Dame, R W, Curley
Rok vydání: 2001
Předmět:
Zdroj: Bioorganicmedicinal chemistry letters. 11(12)
ISSN: 0960-894X
Popis: 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.
Databáze: OpenAIRE