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Total syntheses of the archazolids: an emerging class of novel anticancer drugs
V-ATPase has recently emerged as a promising novel anticancer target based on extensive in vitro and in vivo studies with the archazolids, complex polyketide macrolides which present the most potent V-ATPase inhibitors known to date, rendering these macrolides important lead structures for the devel...
Autores principales: | , |
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Formato: | Online Artículo Texto |
Lenguaje: | English |
Publicado: |
Beilstein-Institut
2017
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Materias: | |
Acceso en línea: | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC5480361/ https://www.ncbi.nlm.nih.gov/pubmed/28684988 http://dx.doi.org/10.3762/bjoc.13.108 |
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author | Scheeff, Stephan Menche, Dirk |
author_facet | Scheeff, Stephan Menche, Dirk |
author_sort | Scheeff, Stephan |
collection | PubMed |
description | V-ATPase has recently emerged as a promising novel anticancer target based on extensive in vitro and in vivo studies with the archazolids, complex polyketide macrolides which present the most potent V-ATPase inhibitors known to date, rendering these macrolides important lead structures for the development of novel anticancer agents. The limited natural supply of these metabolites from their myxobacterial source renders total synthesis of vital importance for the further preclinical development. This review describes in detail the various tactics and strategies employed so far in archazolid syntheses that culminated in three total syntheses and discusses the future synthetic challenges that have to be addressed. |
format | Online Article Text |
id | pubmed-5480361 |
institution | National Center for Biotechnology Information |
language | English |
publishDate | 2017 |
publisher | Beilstein-Institut |
record_format | MEDLINE/PubMed |
spelling | pubmed-54803612017-07-06 Total syntheses of the archazolids: an emerging class of novel anticancer drugs Scheeff, Stephan Menche, Dirk Beilstein J Org Chem Review V-ATPase has recently emerged as a promising novel anticancer target based on extensive in vitro and in vivo studies with the archazolids, complex polyketide macrolides which present the most potent V-ATPase inhibitors known to date, rendering these macrolides important lead structures for the development of novel anticancer agents. The limited natural supply of these metabolites from their myxobacterial source renders total synthesis of vital importance for the further preclinical development. This review describes in detail the various tactics and strategies employed so far in archazolid syntheses that culminated in three total syntheses and discusses the future synthetic challenges that have to be addressed. Beilstein-Institut 2017-06-07 /pmc/articles/PMC5480361/ /pubmed/28684988 http://dx.doi.org/10.3762/bjoc.13.108 Text en Copyright © 2017, Scheeff and Menche https://creativecommons.org/licenses/by/4.0https://www.beilstein-journals.org/bjoc/termsThis is an Open Access article under the terms of the Creative Commons Attribution License (https://creativecommons.org/licenses/by/4.0), which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited. The license is subject to the Beilstein Journal of Organic Chemistry terms and conditions: (https://www.beilstein-journals.org/bjoc/terms) |
spellingShingle | Review Scheeff, Stephan Menche, Dirk Total syntheses of the archazolids: an emerging class of novel anticancer drugs |
title | Total syntheses of the archazolids: an emerging class of novel anticancer drugs |
title_full | Total syntheses of the archazolids: an emerging class of novel anticancer drugs |
title_fullStr | Total syntheses of the archazolids: an emerging class of novel anticancer drugs |
title_full_unstemmed | Total syntheses of the archazolids: an emerging class of novel anticancer drugs |
title_short | Total syntheses of the archazolids: an emerging class of novel anticancer drugs |
title_sort | total syntheses of the archazolids: an emerging class of novel anticancer drugs |
topic | Review |
url | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC5480361/ https://www.ncbi.nlm.nih.gov/pubmed/28684988 http://dx.doi.org/10.3762/bjoc.13.108 |
work_keys_str_mv | AT scheeffstephan totalsynthesesofthearchazolidsanemergingclassofnovelanticancerdrugs AT menchedirk totalsynthesesofthearchazolidsanemergingclassofnovelanticancerdrugs |