Document Report Card

ID: ALA1135685

Journal: J Med Chem

Title: Tumor-specific novel taxoid-monoclonal antibody conjugates.

Authors: Ojima I, Geng X, Wu X, Qu C, Borella CP, Xie H, Wilhelm SD, Leece BA, Bartle LM, Goldmacher VS, Chari RV.

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.

CiteXplore: 12477344

DOI: 10.1021/jm025540g