Using solid phase-assisted synthesis and purification, a 49 member library of analogs of the mammary tumor chemopreventive retinoid N-(4-hydroxyphenyl)retinamide (4-HPR) has been prepared. After prescreening for growth inhibitory activity in human mammary tumor cells (MCF-7) in culture, most of those analogs which showed activity (12 of them) were assayed for apoptosis-inducing activity in the MCF-7 cells. At least 3 of the analogs (13, 24, and 28) showed activity approaching that of 4-HPR.The synthetic retinoid N-(4-hydroxyphenyl)retinamide (4-HPR; 1) was developed a number of years ago and has shown promise as a breast cancer chemopreventive agent in animals.
Supplementary Figure 1 from The Unhydrolyzable Fenretinide Analogue 4-Hydroxybenzylretinone Induces the Proapoptotic Genes <i>GADD153</i> (<i>CHOP</i>) and <i>Bcl-2–Binding Component 3</i> (<i>PUMA</i>) and Apoptosis that Is Caspase- Dependent and Independent of the Retinoic Acid Receptor
scite is a Brooklyn-based organization that helps researchers better discover and understand research articles through Smart Citations–citations that display the context of the citation and describe whether the article provides supporting or contrasting evidence. scite is used by students and researchers from around the world and is funded in part by the National Science Foundation and the National Institute on Drug Abuse of the National Institutes of Health.