Reductively activated disulfide prodrugs of paclitaxel

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. (C) 2002 Elsevier Science Ltd. All rights reserved.