Document Detail

Anti-cancer activity of an acid-labile N-alkylisatin conjugate targeting the transferrin receptor.
MedLine Citation:
PMID:  22115965     Owner:  NLM     Status:  Publisher    
We have previously reported a series of pH-sensitive imine-linked N-alkylisatin prodrugs that are stable at pH 7.4, but readily cleaved at pH 4.5. Herein, one of the most potent prodrugs, 5,7-dibromo-N-(p-methoxybenzyl)isatin (NAI), was functionalized with a para-phenylpropionic acid linker, and the resulting NAI-imine prodrug conjugated to transferrin (Tf) to form a NAI-imine-Tf conjugate. Cytotoxicity assays revealed the conjugate was equipotent to the free drug against MCF-7 breast cancer cells, with clear selectivity patterns based on TfR levels. These results suggest that this novel isatin-based cytotoxin conjugated to a tumor targeting protein via an acid-labile linker warrants further preclinical testing.
Vineesh Indira Chandran; Lidia Matesic; Julie M Locke; Danielle Skropeta; Marie Ranson; Kara L Vine
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Publication Detail:
Type:  JOURNAL ARTICLE     Date:  2011-11-21
Journal Detail:
Title:  Cancer letters     Volume:  -     ISSN:  1872-7980     ISO Abbreviation:  -     Publication Date:  2011 Nov 
Date Detail:
Created Date:  2011-11-25     Completed Date:  -     Revised Date:  -    
Medline Journal Info:
Nlm Unique ID:  7600053     Medline TA:  Cancer Lett     Country:  -    
Other Details:
Languages:  ENG     Pagination:  -     Citation Subset:  -    
Copyright Information:
Copyright © 2011. Published by Elsevier Ireland Ltd.
School of Biological Sciences and Center for Medical Bioscience, University of Wollongong, Northfields Avenue, NSW 2522, Australia; Illawarra Health and Medical Research Institute, University of Wollongong, Northfields Avenue, NSW 2522, Australia.
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