Vrudhula Vivekananda M, MacMaster John F, Li Zhengong, Kerr David E, Senter Peter D
Bristol-Myers Squibb Pharmaceutical Research Institute, 5 Research Parkway, Wallingford, CT 06492, USA.
Bioorg Med Chem Lett. 2002 Dec 16;12(24):3591-4. doi: 10.1016/s0960-894x(02)00784-9.
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.
