Inhibition of reverse transcriptase and Taq DNA polymerase by compounds possessing the coumarin framework |
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| Affiliation: | 1. Inserm U1151, Institut Necker Enfants Malades (INEM), Equipe Physiopathologie des Hormones PRL/GH, Paris, France;2. Sorbonne Paris Cité, Université Paris Descartes, Paris, France;3. Structural Biology and NMR Laboratory, Department of Biology, University of Copenhagen, Copenhagen, Denmark;4. Institut Pasteur, Plateforme de Biophysique des Macromolécules et de leurs Interactions, Département de Biologie Structurale et Chimie, F-75015 Paris, France;5. Laboratoire de Cristallographie et RMN Biologiques CNRS, UMR 8015 Paris, France |
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| 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. |
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| Keywords: | Coumarins Reverse transcriptase Polymerase Molecular target Inhibition |
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