Photoinduced fluorescent cross-linking of 5-chloro- and 5-fluoro-4-thiouridines with thymidine

J Org Chem. 2010 Feb 5;75(3):621-6. doi: 10.1021/jo902136k.

Abstract

Two highly fluorescent, thermally stable diastereomeric photoadducts, 3a,b, are formed when either 5-chloro-4-thiouridine, 1, or 5-fluoro-4-thiouridine, 2, are photoexcited with 366 nm UV light in the presence of thymidine (T). 5-Fluoro-4-thiouridine, 2, exhibits photoreactivity much higher than that of the 5-chloro derivative 1. In both cases the photoreaction is very clean, leading to highly eficient conversion of the 5-halogeno-4-thiouridine (1, 2) and T to photoadducts 3a,b. The identity and structure of 3a was confirmed using mass spectrometry and 2-D NMR. The epimeric relationship of 3a,b was established by UV circular dichroism spectroscopy. The geometry of the fluorescent photoadduct is consistent with formation of an interstrand cross-link in a DNA duplex if 1 or 2 is flanked by T in an opposite strand.

Publication types

  • Research Support, Non-U.S. Gov't
  • Research Support, U.S. Gov't, Non-P.H.S.

MeSH terms

  • Cross-Linking Reagents
  • Crystallography, X-Ray
  • Models, Molecular
  • Molecular Sequence Data
  • Photochemistry
  • Spectrophotometry, Ultraviolet
  • Stereoisomerism
  • Structure-Activity Relationship
  • Thiouridine / analogs & derivatives*
  • Thiouridine / chemistry
  • Thymidine / chemistry*

Substances

  • 5-chloro-4-thiouridine
  • 5-fluoro-4-thiouridine
  • Cross-Linking Reagents
  • Thiouridine
  • Thymidine