Journal
JOURNAL OF MEDICINAL CHEMISTRY
Volume 45, Issue 26, Pages 5620-5623Publisher
AMER CHEMICAL SOC
DOI: 10.1021/jm025540g
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- NIGMS NIH HHS [GM427980] Funding Source: Medline
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Taxoids: bearing methyldisulfanyl(alkanoyl) groups for taxoid-antibody immunoconjugates were designed, synthesized and their activities evaluated. A highly cytotoxic C-10 methyldisuffanylpropanoyl 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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