Design and regioselective synthesis of a new generation of targeted chemotherapeutics. Part 1: EC145, a folic acid conjugate of desacetylvinblastine monohydrazide |
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| Authors: | Vlahov Iontcho R Santhapuram Hari Krishna R Kleindl Paul J Howard Stephen J Stanford Katheryn M Leamon Christopher P |
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| Institution: | Endocyte Inc., 3000 Kent Ave, Suite A1-100, West Lafayette, IN 47906, USA. ivlahov@endocyte.com |
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| Abstract: | An efficient synthesis of the folate receptor (FR) targeting conjugate EC145 is described. EC145 is a water soluble derivative of the vitamin folic acid and the potent cytotoxic agent, desacetylvinblastine monohydrazide. Both molecules are connected in regioselective manner via a hydrophilic peptide spacer and a reductively labile disulfide linker. |
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