RE12 derivatives displaying Vaccinia H1-related phosphatase (VHR) inhibition in the presence of detergent and their anti-proliferative activity against HeLa cells

…, K Oonuma, A Tsuchiya, T Uchida, T Tsuchimoto…

文献索引：Thuaud, Frederic; Kojima, Shuntaro; Hirai, Go; Oonuma, Kana; Tsuchiya, Ayako; Uchida, Takako; Tsuchimoto, Teruhisa; Sodeoka, Mikiko Bioorganic and Medicinal Chemistry, 2014 , vol. 22, # 9 p. 2771 - 2782

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被引用次数: 4

摘要

Abstract New derivatives of Vaccinia H1-related phosphatase (VHR) inhibitor RE12 (5) were designed by replacing the long straight alkyl chain with other hydrophobic functionalities containing two aromatic rings, with the aim of obtaining potent, cell-active inhibitors. We established a direct coupling reaction between tetronic acid derivative and thioimidate to prepare the RE derivatives 6a–6i efficiently. These compounds all showed VHR-inhibitory ...