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.
Rodriquez, M., Cini, E., Petricci, E., D’Ursi, A.M., Saturnino, C., Randino, R. (2014). Tryptophan-based linear dipeptides and 1,4-diketopiperazines as simplified scaffold of the natural cyclotetrapeptide FR235222. PHARMACOLOGYONLINE, 3, 209-215.
Tryptophan-based linear dipeptides and 1,4-diketopiperazines as simplified scaffold of the natural cyclotetrapeptide FR235222
Manuela, Rodriquez;Elena, Cini;Elena, Petricci;Rosario, Randino
2014-01-01
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.
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https://hdl.handle.net/11365/999259
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