Inhibition of reverse transcriptase and Taq DNA polymerase by compounds possessing the coumarin framework

Bioorg Med Chem Lett. 2014 Feb 1;24(3):760-4. doi: 10.1016/j.bmcl.2013.12.104. Epub 2014 Jan 3.

Abstract

Coumarin derivatives were prepared using natural products isolated from plants belonging in the Pterocaulon genus (Asteraceae) and commercial drugs. Some molecules have displayed interesting activity against myeloid murine leukemia virus-reverse transcriptase (MMLV-RT) (compounds 20 and 28 produced inhibition with IC50 values of 38.62 and 50.98 μM, respectively) and Taq DNA polymerase (analogues 13 and 14 produced inhibition with IC50 values of 48.08 and 57.88 μM, respectively). Such inhibitors may have importance as antiretroviral chemotherapeutic agents and also in the development of anticancer drugs.

Keywords: Coumarins; Inhibition; Molecular target; Polymerase; Reverse transcriptase.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Asteraceae / chemistry
  • Cell Line, Tumor
  • Coumarins / chemistry*
  • Coumarins / pharmacology*
  • Enzyme Activation / drug effects
  • Inhibitory Concentration 50
  • Mice
  • Models, Biological
  • Molecular Structure
  • Moloney murine leukemia virus / enzymology
  • Plant Preparations / chemistry
  • Reverse Transcriptase Inhibitors / chemical synthesis
  • Reverse Transcriptase Inhibitors / chemistry*
  • Reverse Transcriptase Inhibitors / pharmacology*
  • Taq Polymerase / antagonists & inhibitors*

Substances

  • Coumarins
  • Plant Preparations
  • Reverse Transcriptase Inhibitors
  • coumarin
  • Taq Polymerase