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

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

文献索引：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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被引用次数: 11

摘要

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 ...