Isoxazolo (aza) naphthoquinones: A new class of cytotoxic Hsp90 inhibitors

A Bargiotti, L Musso, S Dallavalle, L Merlini…

Index: Bargiotti, Alberto; Musso, Loana; Dallavalle, Sabrina; Merlini, Lucio; Gallo, Grazia; Ciacci, Andrea; Giannini, Giuseppe; Cabri, Walter; Penco, Sergio; Vesci, Loredana; Castorina, Massimo; Milazzo, Ferdinando Maria; Cervoni, Maria Luisa; Barbarino, Marcella; Pisano, Claudio; Giommarelli, Chiara; Zuco, Valentina; De Cesare, Michelandrea; Zunino, Franco European Journal of Medicinal Chemistry, 2012 , vol. 53, p. 64 - 75

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Citation Number: 11

Abstract

A series of 3-aryl-naphtho [2, 3–d] isoxazole-4, 9-diones and some of their 6-aza analogues were synthesized and found to inhibit the heat shock protein 90 (Hsp90). The compounds were tested for their binding to Hsp90 and for their effects on Hsp90 client proteins expression in a series of human tumour cell lines. Representative compounds (7f, 10c) downregulated the Hsp90 client proteins EGFR, Akt, Cdk4, Raf-1, and survivin, and ...

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