Abstract
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.
Original language | English |
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Pages (from-to) | 1583-1586 |
Number of pages | 4 |
Journal | Bioorganic and Medicinal Chemistry Letters |
Volume | 11 |
Issue number | 12 |
DOIs | |
State | Published - Jun 18 2001 |
Externally published | Yes |
Funding
Financial support in the form of a grant (CA49837) from the National Cancer Institute is gratefully acknowledged.