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Reductively activated disulfide prodrugs of paclitaxel
Vivekananda M Vrudhula1, John F MacMaster, Zhengong Li
1Bristol-Myers Squibb Pharmaceutical Research Institute, 5 Research Parkway, Wallingford, CT 06492, USA. vrudhula@bms.com
Bioorganic & Medicinal Chemistry Letters
|November 22, 2002
Abstract:
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.