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pKa modulation of a bis(2-aminoimidazoline) DNA minor groove binder that targets the kinetoplast of Trypanosoma brucei

Author
Nué, J.; Millán, C.; Ebiloma, G.; De Koning, H.; Campos, J.Lourdes; Dardonville, C.
Type of activity
Presentation of work at congresses
Name of edition
4th International Electronic Conference on Medicinal Chemistry
Date of publication
2018
Presentation's date
2018-11-03
Book of congress proceedings
Book of abstracts of the 4th International Electronic Conference on Medicinal Chemistry
First page
1
Last page
1
DOI
10.3390/ecmc-4-05626
URL
https://sciforum.net/paper/view/conference/5626 Open in new window
Abstract
The parasite Trypanosoma brucei, ethiologic agent of human African trypanosomiasis (i.e. sleeping sickness), contains a kinetoplast with the mitochondrial DNA (kDNA) comprising of >70 % AT base pairs. Hence, DNA minor groove binding molecules have been investigated as antitrypanosomal agents. Diphenyl-based bis(2-iminoimidazolidines) are promising DNA minor groove binders that are curative in mouse models of stage 1 trypanosomiasis but devoid of activity in the late(CNS)-stage disease, possibly ...
Keywords
DNA minor groove binder, Trypanosoma brucei, dicationic compound, imidazolidine, kinetoplast
Group of research
CEBIM - Molecular Biotechnology Centre
MACROM - Crystallography, Structure and Function of Biological Macromolecules

Participants

  • Nué Martinez, J. Jonathan  (author and speaker )
  • Millán, Cinthia  (author and speaker )
  • Ebiloma, Godwin U.  (author and speaker )
  • De Koning, Harry Pieter  (author and speaker )
  • Campos Lopez, Josefa de Lourdes  (author and speaker )
  • Dardonville, Cristophe Y.  (author and speaker )