1584301-65-4Relevant articles and documents
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,Meli, Maria,Giannini, Giuseppe,Vesci, Loredana,Carollo, Valeria,Brunetti, Tiziana,Battistuzzi, Gianfranco,Tolomeo, Manlio,Cabri, Walter
, p. 53 - 60 (2014/03/21)
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.