Synthesis and evaluation of thymidine-5'-O-monophosphate analogues as inhibitors of Mycobacterium tuberculosis thymidylate kinase.

@article{Vanheusden2002SynthesisAE,
  title={Synthesis and evaluation of thymidine-5'-O-monophosphate analogues as inhibitors of Mycobacterium tuberculosis thymidylate kinase.},
  author={Veerle Vanheusden and H{\'e}l{\'e}ne Munier-Lehmann and Sylvie Pochet and Piet Herdewijn and Serge van Calenbergh},
  journal={Bioorganic & medicinal chemistry letters},
  year={2002},
  volume={12 19},
  pages={2695-8}
}
A number of 2'- and 3'-modified thymidine 5'-O-monophosphate analogues were synthesized as potential leads for new anti-mycobacterial drugs. Evaluation of their affinity for Mycobacterium tuberculosis thymidine monophosphate kinase showed that a 2'-halogeno substituent and a 3'-azido function are the most favorable leads for further development of potent inhibitors of this enzyme.