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Reductively activated disulfide prodrugs of paclitaxel

VM Vrudhula, JF MacMaster, Z Li, DE Kerr…

文献索引:Vrudhula, Vivekananda M; MacMaster, John F; Li, Zhengong; Kerr, David E; Senter, Peter D Bioorganic and medicinal chemistry letters, 2002 , vol. 12, # 24 p. 3591 - 3594

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被引用次数: 55

摘要

A series of unsymmetrical polar disulfide prodrugs 2–5 of paclitaxel were designed and synthesized as reductively activated prodrugs. These compounds behaved as prodrugs in vitro on L2987 lung carcinoma cells. In vivo evaluation in mice demonstrated that the mutual prodrug 5 with captopril exhibited significant regressions and cures.