| Anti-cancer activity of an acid-labile N-alkylisatin conjugate targeting the transferrin receptor. | |
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MedLine Citation:
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PMID: 22115965 Owner: NLM Status: Publisher |
Abstract/OtherAbstract:
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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. |
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Authors:
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Vineesh Indira Chandran; Lidia Matesic; Julie M Locke; Danielle Skropeta; Marie Ranson; Kara L Vine |
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Publication Detail:
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Type: JOURNAL ARTICLE Date: 2011-11-21 |
Journal Detail:
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Title: Cancer letters Volume: - ISSN: 1872-7980 ISO Abbreviation: - Publication Date: 2011 Nov |
Date Detail:
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Created Date: 2011-11-25 Completed Date: - Revised Date: - |
Medline Journal Info:
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Nlm Unique ID: 7600053 Medline TA: Cancer Lett Country: - |
Other Details:
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Languages: ENG Pagination: - Citation Subset: - |
Copyright Information:
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Copyright © 2011. Published by Elsevier Ireland Ltd. |
Affiliation:
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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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From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine
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