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Literature DB >> 12443774

Natural and synthetic geiparvarins are strong and selective MAO-B inhibitors. Synthesis and SAR studies.

Angelo Carotti¹, Antonio Carrieri, Stefano Chimichi, Marco Boccalini, Barbara Cosimelli, Carmela Gnerre, Andrea Carotti, Pierre Alain Carrupt, Bernard Testa.

Abstract

Natural geiparvarin 1 and a number of its analogues were prepared and tested as inhibitors of both monoamine oxidase isoforms, MAO-B and MAO-A. The desmethyl congener 6 of geiparvarin, proved potent and selective MAO-B inhibitor (pIC(50)=7.55 vs 4.62). X-ray crystallography and molecular modelling studies helped the understanding of the observed structure-activity relationships.

Entities: Chemical Gene

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Year: 2002 PMID： 12443774 DOI： 10.1016/s0960-894x(02)00798-9

Source DB: PubMed Journal: Bioorg Med Chem Lett ISSN： 0960-894X Impact factor: 2.823

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Cited

8 in total

1. Cytotoxic activity of new acetoxycoumarin derivatives in cancer cell lines.

Authors: Musiliyu A Musa; Veera L D Badisa; Lekan M Latinwo; John Cooperwood; Andre Sinclair; Ahkinyala Abdullah
Journal: Anticancer Res Date: 2011-06 Impact factor: 2.480

2. Docking of novel reversible monoamine oxidase-B inhibitors: efficient prediction of ligand binding sites and estimation of inhibitors thermodynamic properties.

Authors: K Yelekçi; O Karahan; M Toprakçi
Journal: J Neural Transm (Vienna) Date: 2007-03-31 Impact factor: 3.575

Review 3. Natural Products Inhibitors of Monoamine Oxidases-Potential New Drug Leads for Neuroprotection, Neurological Disorders, and Neuroblastoma.

Authors: Narayan D Chaurasiya; Francisco Leon; Ilias Muhammad; Babu L Tekwani
Journal: Molecules Date: 2022-07-04 Impact factor: 4.927

Natural and synthetic geiparvarins are strong and selective MAO-B inhibitors. Synthesis and SAR studies.

1. Cytotoxic activity of new acetoxycoumarin derivatives in cancer cell lines.

2. Docking of novel reversible monoamine oxidase-B inhibitors: efficient prediction of ligand binding sites and estimation of inhibitors thermodynamic properties.

Review 3. Natural Products Inhibitors of Monoamine Oxidases-Potential New Drug Leads for Neuroprotection, Neurological Disorders, and Neuroblastoma.

Review 4. A review of coumarin derivatives in pharmacotherapy of breast cancer.

5. Binding models of reversible inhibitors to type-B monoamine oxidase.

6. New solid phase methodology for the synthesis of biscoumarin derivatives: experimental and in silico approaches.

Review 7. Coumarin: A Natural, Privileged and Versatile Scaffold for Bioactive Compounds.

8. Side-chain modifications of highly functionalized 3(2H)-furanones.