Back to Search
Start Over
DNA minor groove binders-inspired by nature
- Source :
- Acta Chimica Slovenica, Vol 63, Iss 4, Pp 689-704 (2016), Acta chimica slovenica
- Publication Year :
- 2016
-
Abstract
- 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.
- Subjects :
- 0301 basic medicine
Magnetic Resonance Spectroscopy
Stereochemistry
Lexitropsin
DNA Footprinting
DNA footprinting
Trypanosoma brucei
RS
lcsh:Chemistry
03 medical and health sciences
chemistry.chemical_compound
Animals
Humans
Computer Simulation
QD
030102 biochemistry & molecular biology
biology
Minor Groove Binders
Chemistry
Distamycins
Biological activity
Netropsin
DNA
Nuclear magnetic resonance spectroscopy
Clostridium difficile
biology.organism_classification
Trypanocidal Agents
Distamycin
Footprinting
Anti-Bacterial Agents
Antibacterial
Biochemistry
lcsh:QD1-999
Thiazotropsin A
Subjects
Details
- Language :
- English
- ISSN :
- 13180207
- Database :
- OpenAIRE
- Journal :
- Acta Chimica Slovenica, Vol 63, Iss 4, Pp 689-704 (2016), Acta chimica slovenica
- Accession number :
- edsair.doi.dedup.....50b6221f0f0049b0a81d0fb44fcace87