DNA Minor Groove Binders-Inspired by Nature

The synthesis and biological activity of a variety of analogues to the naturally occurring antibacterial and antifungal Distamycin A were explored by a number of authors. These compounds were subject to a large array of assays. Some of these compounds showed high activity against a range of Gram-pos...

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Bibliographic Details
Published inActa chimica Slovenica Vol. 63; no. 4; pp. 689 - 704
Main Authors Khalaf, Abedawn Ibrahim, Al-Kadhimi, Ahmed A. H., Ali, Jaafar H.
Format Journal Article
LanguageEnglish
Published Slovenia Slovenian Chemical Society 01.12.2016
Subjects
Animals
Anti-Bacterial Agents - chemistry
Anti-Bacterial Agents - metabolism
Anti-Bacterial Agents - pharmacology
Antibacterial
Clostridium difficile
Computer Simulation
Distamycin
Distamycins - chemistry
Distamycins - metabolism
Distamycins - pharmacology
DNA - chemistry
DNA - metabolism
DNA Footprinting
Humans
Magnetic Resonance Spectroscopy
Minor Groove Binders
Netropsin
Thiazotropsin A
Trypanocidal Agents - chemistry
Trypanocidal Agents - metabolism
Trypanocidal Agents - pharmacology
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Summary:The synthesis and biological activity of a variety of analogues to the naturally occurring antibacterial and antifungal Distamycin A were explored by a number of authors. These compounds were subject to a large array of assays. Some of these compounds showed high activity against a range of Gram-positive, Gram-negative bacteria as well as fungi. To explore the anti-parasitic activity of this class of compounds, specific modifications had to be made. A number of these compounds proved to be active against Trypanosoma brucei. The binding of a number of these compounds to short sequences of DNA were also examined using footprinting assays as well as NMR spectroscopy. Computer modelling was employed on selected compounds to understand the way these compounds bind to specific DNA sequences. A large number of variations were made to the standard structure of Distamycin. These changes involved the replacement of the pyrrole moieties as well as the head and tail groups with a number of heterocyclic compounds. Some of these minor groove binders (MGBs) were also investigated for their capability for the treatment of cancer and in particular lung cancer.
Bibliography:ObjectType-Article-2
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ISSN:1318-0207
1580-3155
DOI:10.17344/acsi.2016.2775