Chiral discrimination in binding of enantiomers of 2-(aminoalkoxy)-substituted 4-(2-thienyl)pyrimidines and 4,6-bis(2-thienyl)pyrimidines with duplex DNA

Separation of fudosteine on an achiral C18column by HPLC with chiral ligand-exchange selectors as mobile phase additives

“…Administration of highly pure chiral drugs is therefore a major objective of the pharmaceutical industry to protect the public against damage caused by high drug concentrations or toxic side-effects. Chiral discrimination is, therefore, an issue in drug development [4][5][6][7][8][9]. The literature is rich in analytical methods for analysis of fudosteine [10][11][12][13][14] but methods for separation of the enantiomers of fudosteine were few.…”

Sequence and Chiral Selectivity of Drug–DNA Interactions Revealed by Force Spectroscopy

“…2 Among the most important aspects in characterizing these systems are the sequence selectivity of the DNA and the conformational selectivity of the drug molecules. Various techniques have been extensively applied to study drug–DNA systems, including NMR spectroscopy,3, 4 second harmonic generation,5 fluorescence spectroscopy,6, 7 circular dichroism,8 UV melting,9 X‐ray diffraction,10 magnetic tweezers,11 atomic force microscopy (AFM),12, 13 and optical tweezers 14–16. It remains challenging, however, to directly measure the binding strength of such interactions with sufficiently high force resolution, so that different drug–DNA interactions can be distinguished.…”

“…The first experiment to validate this concept was carried out with the T‐Hg‐T system, where T=thymine and Hg=Hg 2+ . This system has been well studied by NMR spectroscopy as well as other spectroscopic techniques 4. 6, 20–22 It is thus well‐known that Hg specifically intercalates into a DNA duplex at the T‐T mismatching pair.…”