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Serine- and Threonine-derived Diamine Equivalents for Site-specific Incorporation of Platinum Centers in Peptides, and Anticancer Potential of these Conjugates

Abstract

A modular strategy that allows introduction of one or more reactive platinum units at chosen locations along a peptide sequence is presented. This makes use of diazides generated from serine and threonine as diamine equivalents which can be conjugated to the peptide under standard coupling condition. Reduction of these diazides using Pd/C, H2 followed by platination affords the final products in good yields. Following this we have prepared a new class of peptide-platinum conjugates and have carried out preliminary cytotoxicity evaluation and DNA interaction studies. Inclusion of lysine residues in the sequence was found to improve DNA interaction as well as anticancer activities compared to analogous conjugates with hydrophobic side chains.

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Publication details

The article was received on 17 Oct 2017, accepted on 05 Jan 2018 and first published on 08 Jan 2018


Article type: Paper
DOI: 10.1039/C7NJ03999A
Citation: New J. Chem., 2018, Accepted Manuscript
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    Serine- and Threonine-derived Diamine Equivalents for Site-specific Incorporation of Platinum Centers in Peptides, and Anticancer Potential of these Conjugates

    M. K. Manheri, S. Kumbhakonam, K. Vellaisamy, S. Saroj, N. Venkatesan and K. Devarajan, New J. Chem., 2018, Accepted Manuscript , DOI: 10.1039/C7NJ03999A

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