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 R., Simoni D., Marchetti P., Rondanin R., Mangiola S., Costantini C:, et al. (2014). 4,5,6,7-Tetrahydro-isoxazolo-[4,5-c]-pyridines as a new class of cytotoxic Hsp90 inhibitors. EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY, 76, 53-60 [10.1016/j.ejmech.2014.01.056].

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

Cabri W
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.
2014
Baruchello R., Simoni D., Marchetti P., Rondanin R., Mangiola S., Costantini C:, et al. (2014). 4,5,6,7-Tetrahydro-isoxazolo-[4,5-c]-pyridines as a new class of cytotoxic Hsp90 inhibitors. EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY, 76, 53-60 [10.1016/j.ejmech.2014.01.056].
Baruchello R.; Simoni D.; Marchetti P.; Rondanin R.; Mangiola S.; Costantini C:; Meli M.; Giannini G:; Vesci L.; Carollo V.; Brunetti T.; Battistuzzi...espandi
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Utilizza questo identificativo per citare o creare un link a questo documento: https://hdl.handle.net/11585/756812
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