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Design, Synthesis and Biological Evaluation of Highly Potent Simplified Archazolids
The archazolids are potent antiproliferative compounds that have recently emerged as a novel class of promising anticancer agents. Their complex macrolide structures and scarce natural supply make the development of more readily available analogues highly important. Herein, we report the design, syn...
Autores principales: | , , , , , , , |
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Formato: | Online Artículo Texto |
Lenguaje: | English |
Publicado: |
John Wiley and Sons Inc.
2020
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Materias: | |
Acceso en línea: | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7496434/ https://www.ncbi.nlm.nih.gov/pubmed/32363789 http://dx.doi.org/10.1002/cmdc.202000154 |
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author | Rivière, Solenne Vielmuth, Christin Ennenbach, Christiane Abdelrahman, Aliaa Lemke, Carina Gütschow, Michael Müller, Christa E. Menche, Dirk |
author_facet | Rivière, Solenne Vielmuth, Christin Ennenbach, Christiane Abdelrahman, Aliaa Lemke, Carina Gütschow, Michael Müller, Christa E. Menche, Dirk |
author_sort | Rivière, Solenne |
collection | PubMed |
description | The archazolids are potent antiproliferative compounds that have recently emerged as a novel class of promising anticancer agents. Their complex macrolide structures and scarce natural supply make the development of more readily available analogues highly important. Herein, we report the design, synthesis and biological evaluation of four simplified and partially saturated archazolid derivatives. We also reveal important structure‐activity relationship data as well as insights into the pharmacophore of these complex polyketides. |
format | Online Article Text |
id | pubmed-7496434 |
institution | National Center for Biotechnology Information |
language | English |
publishDate | 2020 |
publisher | John Wiley and Sons Inc. |
record_format | MEDLINE/PubMed |
spelling | pubmed-74964342020-09-25 Design, Synthesis and Biological Evaluation of Highly Potent Simplified Archazolids Rivière, Solenne Vielmuth, Christin Ennenbach, Christiane Abdelrahman, Aliaa Lemke, Carina Gütschow, Michael Müller, Christa E. Menche, Dirk ChemMedChem Full Papers The archazolids are potent antiproliferative compounds that have recently emerged as a novel class of promising anticancer agents. Their complex macrolide structures and scarce natural supply make the development of more readily available analogues highly important. Herein, we report the design, synthesis and biological evaluation of four simplified and partially saturated archazolid derivatives. We also reveal important structure‐activity relationship data as well as insights into the pharmacophore of these complex polyketides. John Wiley and Sons Inc. 2020-06-10 2020-07-20 /pmc/articles/PMC7496434/ /pubmed/32363789 http://dx.doi.org/10.1002/cmdc.202000154 Text en © 2020 The Authors. Published by Wiley-VCH Verlag GmbH & Co. KGaA. This is an open access article under the terms of the http://creativecommons.org/licenses/by/4.0/ License, which permits use, distribution and reproduction in any medium, provided the original work is properly cited. |
spellingShingle | Full Papers Rivière, Solenne Vielmuth, Christin Ennenbach, Christiane Abdelrahman, Aliaa Lemke, Carina Gütschow, Michael Müller, Christa E. Menche, Dirk Design, Synthesis and Biological Evaluation of Highly Potent Simplified Archazolids |
title | Design, Synthesis and Biological Evaluation of Highly Potent Simplified Archazolids |
title_full | Design, Synthesis and Biological Evaluation of Highly Potent Simplified Archazolids |
title_fullStr | Design, Synthesis and Biological Evaluation of Highly Potent Simplified Archazolids |
title_full_unstemmed | Design, Synthesis and Biological Evaluation of Highly Potent Simplified Archazolids |
title_short | Design, Synthesis and Biological Evaluation of Highly Potent Simplified Archazolids |
title_sort | design, synthesis and biological evaluation of highly potent simplified archazolids |
topic | Full Papers |
url | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7496434/ https://www.ncbi.nlm.nih.gov/pubmed/32363789 http://dx.doi.org/10.1002/cmdc.202000154 |
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