DNA minor groove binders-inspired by nature

Abedawn I. Khalaf, Ahmed A. H Al-Khadhimi, Jaafar H. Ali

Research output: Contribution to journalArticle

7 Citations (Scopus)
61 Downloads (Pure)

Abstract

The synthesis and biological activity of a variety of analogues to the naturally occurring anti-bacterial and anti-fungal 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 MGBs were also investigated for their capability for the treatment of cancer and in particular lung cancer.
Original languageEnglish
Pages (from-to)689–704
Number of pages16
JournalActa Chimica Slovenica
Volume63
Issue number4
DOIs
Publication statusPublished - 8 Dec 2016

Keywords

  • minor groove binders
  • distamycin
  • netropsin
  • antibacterial
  • Thiazotropsin A
  • Clostridium difficile
  • Lexitropsins
  • deoxyribonucleic acid
  • DNA binding ligands

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