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MARIA MELI

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

  • Autori: Baruchello, R.; Simoni, D.; Marchetti, P.; Rondanin, R.; Mangiola, S.; Costantini, C.; Meli, M.; Giannini, G.; Vesci, L.; Carollo, V.; Brunetti, T.; Battistuzzi, G.; Tolomeo, M.; Cabri, W.
  • Anno di pubblicazione: 2014
  • Tipologia: Articolo in rivista (Articolo in rivista)
  • OA Link: http://hdl.handle.net/10447/90523

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.