Structural studies on bioactive compounds. Part 26. Hydrogen bonding in the crystal structure of the N-methylformamide solvate of the immunomodulatory agent 2-amino-5-bromo-6-phenylpyrimidin-4-one (bropirimine): implications for the design of novel anti-tumour strategies

Anticancer Drug Des. 1995 Apr;10(3):203-13.

Abstract

The immunomodulatory agent bropirimine crystallizes from N-methylformamide (NMF) as a triply hydrogen-bonded duplex in the manner of a Watson-Crick guanine:cytosine base pair. The stoichiometry of the solvate is bropirimine:NMF (2:1) and all NMF molecules are in the Z-rotomeric form. The intermolecular hydrogen bonding is disrupted when the solvate is dissolved in deuteriated dimethyl sulphoxide at 37 degrees C. Bropirimine and other molecules which possess the 2-aminopyrimidin-4-one fragment are potentially capable of recognizing guanine or cytosine residues in single-stranded RNA or DNA by Watson-Crick bonding or double-stranded DNA by Hoogsteen bonds. The immunomodulatory properties of these compounds might be triggered by these encounters.

MeSH terms

  • Adjuvants, Immunologic / chemistry*
  • Adjuvants, Immunologic / pharmacology
  • Crystallography, X-Ray
  • Cytosine / analogs & derivatives*
  • Cytosine / chemistry
  • Cytosine / pharmacology
  • Drug Design*
  • Formamides / chemistry*
  • Hydrogen Bonding
  • Magnetic Resonance Spectroscopy
  • Molecular Structure
  • Solvents

Substances

  • Adjuvants, Immunologic
  • Formamides
  • Solvents
  • Cytosine
  • bropirimine
  • methylformamide