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J Med Chem. 2002 Dec 19;45(26):5620-3.

Tumor-specific novel taxoid-monoclonal antibody conjugates.

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  • 1Department of Chemistry, State University of New York at Stony Brook, Stony Brook, New York 11794-3400, USA.


Taxoids bearing methyldisulfanyl(alkanoyl) groups for taxoid-antibody immunoconjugates were designed, synthesized and their activities evaluated. A highly cytotoxic C-10 methyldisulfanylpropanoyl taxoid was conjugated to monoclonal antibodies recognizing the epidermal growth factor receptor (EGFR) expressed in human squamous cancers. These conjugates were shown to possess remarkable target-specific antitumor activity in vivo against EGFR-expressing A431 tumor xenografts in severe combined immune deficiency mice, resulting in complete inhibition of tumor growth in all the treated mice.

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