Synthesis, Characterization and anti-HIV and Antitumor Activities of New Coumarin Derivatives

Yaseen A. Al-Soud 1 , Haitham H. Al-Sa’doni 1 , Houssain A. S. Amajaour 1 , Kifah S. M. Salih 2 , Mohammad S. Mubarakb 2  and Najim A. Al-Masoudic 3
  • 1 Department of Chemistry, College of Science, University of Al al-Bayt, Al-Mafraq, Jordan
  • 2 Department of Chemistry, Faculty of Science, University of Jordan, Amman, Jordan
  • 3 Formerly Fachbereich Chemie, Universität Konstanz, D-78457 Konstanz, Germany

A new series of coumarin and benzofuran derivatives were synthesized as potential non-nucleoside reverse transcriptase inhibitors (NNRTIs) by reacting, separately, 4-bromomethylcoumarins, their sulphonyl chlorides, and ethyl 3-(bromomethyl)-6-methoxy-1-benzofuran-2-carboxylate with different imidazoles and their benzo analogs. The antiviral (HIV-1, HIV-2) properties of the newly synthesized compounds were investigated in vitro and all compounds were found to be inactive, except 10 which showed inhibition of HIV-2 with EC50 > 0.51 μgmL−1. The in vitro cytotoxicity of 17 and 19 was assayed against a panel of tumor cell lines consisting of CD4 human T-cells.

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Zeitschrift für Naturforschung B is an international scientific journal which publishes original papers, microreviews, and letters from all areas of inorganic chemistry, solid state chemistry, coordination chemistry, molecular chemistry, and organic chemistry.