Design and synthesis of novel bis-thiazolone derivatives as micromolar CDC25 phosphatase inhibitors: Effect of dimerisation on phosphatase inhibition

…, MA Miteva, BO Villoutreix, C Garbay, E Braud

Index: Sarkis, Manal; Tran, Diem Ngan; Kolb, Stephanie; Miteva, Maria A.; Villoutreix, Bruno O.; Garbay, Christiane; Braud, Emmanuelle Bioorganic and Medicinal Chemistry Letters, 2012 , vol. 22, # 24 p. 7345 - 7350

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Citation Number: 22

Abstract

CDC25 phosphatases are involved in deregulated cell cycle progression and tumor development with poor prognosis. Among the most potent CDC25 inhibitors, quinonoid- based derivatives have been extensively studied. Dimerisation of heterocyclic quinones has led to IRC-083864, a bis-quinone compound with increased CDC25B inhibitory activity. Thirty-one bis-thiazolone derivatives were synthesized and assayed for CDC25 inhibitory ...