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Selective anti-malarial minor groove binders.

Fraser J Scott1, Abedawn I Khalaf1, Sandra Duffy2

  • 1WestCHEM Department of Pure and Applied Chemistry, University of Strathclyde, 295 Cathedral Street, Glasgow G1 1XL, United Kingdom.

Bioorganic & Medicinal Chemistry Letters
|May 24, 2016
PubMed
Summary

New DNA minor groove binders (MGBs) show promise as antimalarial drugs. These compounds are effective against both drug-sensitive and drug-resistant Plasmodium falciparum strains, offering hope for malaria treatment.

Keywords:
Antimalarial drugDNA minor groove binderPlasmodium falciparum

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Area of Science:

  • Medicinal Chemistry
  • Parasitology
  • Drug Discovery

Background:

  • Malaria remains a significant global health challenge, exacerbated by increasing drug resistance in Plasmodium falciparum.
  • DNA minor groove binders (MGBs) are a class of compounds with potential antimalarial activity.
  • Developing new drugs effective against resistant strains is crucial.

Purpose of the Study:

  • To evaluate a diverse set of 31 DNA minor groove binders (MGBs) for their antimalarial activity against Plasmodium falciparum.
  • To assess the toxicity of these MGBs in mammalian cells.
  • To identify structural features associated with potent and selective antimalarial activity.

Main Methods:

  • Antimalarial activity was tested against chloroquine-sensitive (3D7) and chloroquine-resistant (Dd2) strains of P. falciparum.
  • Mammalian cell toxicity was evaluated using human embryonic kidney (HEK) cells.
  • Structure-activity relationships were analyzed, considering physical chemical properties like logD7.4 and specific structural motifs (e.g., alkene link, C-alkylthiazole).

Main Results:

  • MGBs with an alkene linker between N-terminal building blocks exhibited high activity (IC50: 30-500nM) and therapeutic ratios (>10->500).
  • Compounds containing a C-alkylthiazole moiety were frequently found among the active agents.
  • Effective compounds were identified with logD7.4 values around 3 or 7.
  • Crucially, tested MGBs showed similar efficacy against both sensitive and resistant parasite strains.

Conclusions:

  • Suitably designed DNA minor groove binders (MGBs) demonstrate significant potential as antimalarial drug candidates.
  • These MGBs are effective against drug-resistant Plasmodium falciparum strains, addressing a critical unmet need.
  • Further development of these MGBs could lead to new clinical treatments for malaria.