Loughborough University
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DNA binding studies of fluorinated bioactive heterocyclic compounds

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posted on 2015-02-13, 14:32 authored by Mariam Mojally
Fluorinated heterocyclic compounds have drug like properties and possess a valuable biological activity due to their rigid chemical structures and the high solubility profile. Novel fluorinated heteroarenes have been synthesised by SNAr reaction of a range of fluorinated arenes including pentafluoropyridine, hexafluorobenzene and pentafluorotoluene to introduce a range of groups specially nitriles, benzimidazole, carbazole and benzimidazole. A number of cyclization reactions have been investigated with the aim of forming polycyclic structures that could act as DNA intercalators. The synthesised compounds have been characterized by elemental analysis, IR, 1H and 19F NMR spectroscopy and single crystal analysis. These compounds have been screened for their biological activities including DNA thermal denaturation assay, UV-Visible spectroscopy, fluorescence spectroscopy, X-ray co-crystallization and antimicrobial activity study. Some of the compounds showed potential DNA bonding activity in particular the carbazole derivatives.


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© Mariam Mojally

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This work is made available according to the conditions of the Creative Commons Attribution-NonCommercial-NoDerivatives 4.0 International (CC BY-NC-ND 4.0) licence. Full details of this licence are available at: https://creativecommons.org/licenses/by-nc-nd/4.0/

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A Doctoral Thesis. Submitted in partial fulfilment of the requirements for the award of Doctor of Philosophy of Loughborough University.


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