1. Endocyte Inc., 3000 Kent Ave., Suite A1-100, West Lafayette, IN 47906, USA;2. Bristol-Myers Squibb Research, PO Box 4000, Princeton, NJ 08543, USA
Abstract:
Efficient regioselective syntheses of conjugates of folic acid and cytotoxic agents derived from natural epothilones are described. These folate receptor (FR) targeting compounds are water soluble and incorporate a hydrophilic peptide-based spacer unit and a reducible self-immolative disulfide-based linker system between the FR-targeting ligand and the parent drug.