Tumor-Specific Novel Taxoid−Monoclonal Antibody Conjugates
- 20 November 2002
- journal article
- letter
- Published by American Chemical Society (ACS) in Journal of Medicinal Chemistry
- Vol. 45 (26) , 5620-5623
- https://doi.org/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.Keywords
This publication has 7 references indexed in Scilit:
- Recent Advances in the Medicinal Chemistry of Taxoids with Novel P-Amino Acid Side ChainsCurrent Medicinal Chemistry, 1999
- Recent advances in the medicinal chemistry of taxoid anticancer agentsPublished by Elsevier ,1999
- Selective Deesterification Studies on Taxanes: Simple and Efficient Hydrazinolysis of C-10 and C-13 Ester FunctionalitiesThe Journal of Organic Chemistry, 1995
- New and efficient approaches to the semisynthesis of taxol and its C-13 side chain analogs by means of β-lactam synthon methodTetrahedron, 1992
- Toxicity of ligand and antibody‐directed ricin A‐chain conjugates recognizing the epidermal growth factor receptorJournal of Cellular Physiology, 1987
- Monoclonal antibody against epidermal growth factor receptor is internalized without stimulating receptor phosphorylation.Proceedings of the National Academy of Sciences, 1986
- Promotion of microtubule assembly in vitro by taxolNature, 1979