Hsp90 is considered an interesting therapeutic target for anticancer drug development. Here we describe a new class of 4,5,6,7-tetrahydro-isoxazolo-[4,5-c]-pyridine compounds. A small library of derivatives has been synthesized and investigated. Some reported compounds show interesting properties combining both notable binding to Hsp90 and potent cell growth inhibitory activity. N-5 substitution with a 2,4 resorcinol carboxamide appears crucial for activity. Moreover, a derivative bearing a hydroxamic acid residue bound to C-3 amide portion was found to inhibit both Hsp90 and HDAC6.

4,5,6,7-Tetrahydro-isoxazolo-[4,5-c]-pyridines as a new class of cytotoxic Hsp90 inhibitors

BARUCHELLO, Riccardo;SIMONI, Daniele;MARCHETTI, Paolo;RONDANIN, Riccardo;MANGIOLA, Stefania;COSTANTINI, Cristiana;
2014

Abstract

Hsp90 is considered an interesting therapeutic target for anticancer drug development. Here we describe a new class of 4,5,6,7-tetrahydro-isoxazolo-[4,5-c]-pyridine compounds. A small library of derivatives has been synthesized and investigated. Some reported compounds show interesting properties combining both notable binding to Hsp90 and potent cell growth inhibitory activity. N-5 substitution with a 2,4 resorcinol carboxamide appears crucial for activity. Moreover, a derivative bearing a hydroxamic acid residue bound to C-3 amide portion was found to inhibit both Hsp90 and HDAC6.
Baruchello, Riccardo; Simoni, Daniele; Marchetti, Paolo; Rondanin, Riccardo; Mangiola, Stefania; Costantini, Cristiana; M., Meli; G., Giannini; L., Vesci; V., Carollo; T., Brunetti; G., Battistuzzi; M., Tolomeo; W., Cabri
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Utilizza questo identificativo per citare o creare un link a questo documento: https://hdl.handle.net/11392/2121014
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