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Design and regioselective synthesis of a new generation of targeted chemotherapeutics. Part II: Folic acid conjugates of tubulysins and their hydrazides. | LitMetric
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Design and regioselective synthesis of a new generation of targeted chemotherapeutics. Part II: Folic acid conjugates of tubulysins and their hydrazides.

Iontcho R Vlahov Yu Wang Paul J Kleindl Christopher P Leamon

Bioorg Med Chem Lett

Endocyte Inc., 3000 Kent Avenue, Suite A1-100, West Lafayette, IN 47906, USA.

Published: August 2008

Efficient syntheses of folate conjugates of tubulysins and their hydrazides 1a-d are described. These water soluble folate receptor (FR) targeted conjugates are derivatives of folic acid and the potent cytotoxic agents: tubulysin A, B, or their respective hydrazides, connected in regioselective manner via a hydrophilic peptide spacer and a reducible disulfide linker.

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 Source
http://dx.doi.org/10.1016/j.bmcl.2008.07.041DOI Listing

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