Design, synthesis and biological evaluation of simplified linear and cyclic peptidomimetic analogues of FR235222 (1), natural immunosuppressant and HDAC inhibitor, bearing hydroxyketone moiety as more stable zinc binding group, have been reported. Linear dipeptides (6a-b) show significant antiproliferative activities and are chosen to be promising lead compounds for further optimization, in order to elucidate molecule-enzyme surface recognition.
TRYPTOPHAN-BASED LINEAR DIPEPTIDES AND 1,4-DIKETOPIPERAZINES AS SIMPLIFIED SCAFFOLDS OF THE NATURAL CYCLOTETRAPEPTIDE FR235222 / Rodriquez, Manuela; Elena, Cini; Elena, Petricci; D'Ursi, Anna Maria; Saturnino, Carmela; Randino, Rosario. - In: PHARMACOLOGYONLINE. - ISSN 1827-8620. - 3:(2014), pp. 209-215.
TRYPTOPHAN-BASED LINEAR DIPEPTIDES AND 1,4-DIKETOPIPERAZINES AS SIMPLIFIED SCAFFOLDS OF THE NATURAL CYCLOTETRAPEPTIDE FR235222
RODRIQUEZ, Manuela;
2014
Abstract
Design, synthesis and biological evaluation of simplified linear and cyclic peptidomimetic analogues of FR235222 (1), natural immunosuppressant and HDAC inhibitor, bearing hydroxyketone moiety as more stable zinc binding group, have been reported. Linear dipeptides (6a-b) show significant antiproliferative activities and are chosen to be promising lead compounds for further optimization, in order to elucidate molecule-enzyme surface recognition.| File | Dimensione | Formato | |
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