Issue 4, 2015
From the journal:

MedChemComm

O-Benzoyl pyridine aldoxime and amidoxime derivatives: novel efficient DNA photo-cleavage agents†

Paraskevi Karamtzioti,‡a   Asterios Papastergiou,‡a   John G. Stefanakis,b   Alexandros E. Koumbis,b   Ioanna Anastasiou,a   Maria Koffaa  and  Konstantina C. Fylaktakidou*a  

* Corresponding authors

a Laboratory of Organic, Bioorganic and Natural Product Chemistry, Molecular Biology and Genetics Department, Democritus University of Thrace, University Campus, Dragana, Alexandroupolis, Greece
E-mail: kfylakta@mbg.duth.gr
Fax: +30 25510 30613

b Laboratory of Organic Chemistry, Chemistry Department, Aristotle University of Thessaloniki, Thessaloniki, Greece

Abstract

O-Benzoyl derivatives of meta-, ortho- and para-pyridine aldoximes and amidoximes are novel efficient DNA photo-cleavage agents. In particular O-p-nitro-benzoyl derivatives 4, 8 and 15 were effective at concentrations as low as 1 μM. Both aldoximes and amidoximes were active under aerobic and anaerobic conditions, with a double-stranded to single-stranded DNA cleavage ratio of up to 1. These results give prospects for multiple applications, including phototherapeutic treatment of solid tumors.

Graphical abstract: O-Benzoyl pyridine aldoxime and amidoxime derivatives: novel efficient DNA photo-cleavage agents

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Article information

DOI
https://doi.org/10.1039/C4MD00548A
Article type
Concise Article
Submitted
08 Dec 2014
Accepted
14 Jan 2015
First published
15 Jan 2015

Med. Chem. Commun., 2015,6, 719-726

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O-Benzoyl pyridine aldoxime and amidoxime derivatives: novel efficient DNA photo-cleavage agents

P. Karamtzioti, A. Papastergiou, J. G. Stefanakis, A. E. Koumbis, I. Anastasiou, M. Koffa and K. C. Fylaktakidou, Med. Chem. Commun., 2015, 6, 719 DOI: 10.1039/C4MD00548A

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