2. Academic Validation
  3. Tumor-specific novel taxoid-monoclonal antibody conjugates

Tumor-specific novel taxoid-monoclonal antibody conjugates

  • J Med Chem. 2002 Dec 19;45(26):5620-3. doi: 10.1021/jm025540g.
Iwao Ojima 1,  Xudong Geng,  Xinyuan Wu,  Chuanxing Qu,  Christopher P Borella,  Hongsheng Xie,  Sharon D Wilhelm,  Barbara A Leece,  Laura M Bartle,  Victor S Goldmacher,  Ravi V J Chari
Affiliations

Affiliation

  • 1 Department of Chemistry, State University of New York at Stony Brook, Stony Brook, New York 11794-3400, USA. iojima@notes.cc.sunysb.edu
PMID: 12477344 DOI: 10.1021/jm025540g
Abstract

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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