2. Academic Validation
  3. Reductively activated disulfide prodrugs of paclitaxel

Reductively activated disulfide prodrugs of paclitaxel

  • Bioorg Med Chem Lett. 2002 Dec 16;12(24):3591-4. doi: 10.1016/s0960-894x(02)00784-9.
Vivekananda M Vrudhula 1,  John F MacMaster,  Zhengong Li,  David E Kerr,  Peter D Senter
Affiliations

Affiliation

  • 1 Bristol-Myers Squibb Pharmaceutical Research Institute, 5 Research Parkway, Wallingford, CT 06492, USA. [email protected]
PMID: 12443783 DOI: 10.1016/s0960-894x(02)00784-9
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.

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