A Facile Semisynthesis and Evaluation of Garcinoic Acid and Its Analogs for the Inhibition of Human DNA Polymerase β

Garcinoic acid has been identified as an inhibitor of DNA polymerase β (pol β). However, no structure-activity relationship (SAR) studies of garcinoic acid as a pol β inhibitor have been conducted, in part due to the lack of an efficient synthetic method for this natural product and its analogs. We...

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Autores principales: Gujarathi, Satheesh, Zafar, Maroof Khan, Liu, Xingui, Eoff, Robert L., Zheng, Guangrong
Formato: Online Artículo Texto
Lenguaje:English
Publicado: MDPI 2020
Materias:
Article
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7763917/
https://www.ncbi.nlm.nih.gov/pubmed/33322249
http://dx.doi.org/10.3390/molecules25245847
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author Gujarathi, Satheesh
Zafar, Maroof Khan
Liu, Xingui
Eoff, Robert L.
Zheng, Guangrong
author_facet Gujarathi, Satheesh
Zafar, Maroof Khan
Liu, Xingui
Eoff, Robert L.
Zheng, Guangrong
author_sort Gujarathi, Satheesh
collection PubMed
description Garcinoic acid has been identified as an inhibitor of DNA polymerase β (pol β). However, no structure-activity relationship (SAR) studies of garcinoic acid as a pol β inhibitor have been conducted, in part due to the lack of an efficient synthetic method for this natural product and its analogs. We developed an efficient semi-synthetic method for garcinoic acid and its analogs by starting from natural product δ-tocotrienol. Our preliminary SAR studies provided a valuable insight into future discovery of garcinoic acid-based pol β inhibitors.
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spelling pubmed-77639172020-12-27 A Facile Semisynthesis and Evaluation of Garcinoic Acid and Its Analogs for the Inhibition of Human DNA Polymerase β Gujarathi, Satheesh Zafar, Maroof Khan Liu, Xingui Eoff, Robert L. Zheng, Guangrong Molecules Article Garcinoic acid has been identified as an inhibitor of DNA polymerase β (pol β). However, no structure-activity relationship (SAR) studies of garcinoic acid as a pol β inhibitor have been conducted, in part due to the lack of an efficient synthetic method for this natural product and its analogs. We developed an efficient semi-synthetic method for garcinoic acid and its analogs by starting from natural product δ-tocotrienol. Our preliminary SAR studies provided a valuable insight into future discovery of garcinoic acid-based pol β inhibitors. MDPI 2020-12-11 /pmc/articles/PMC7763917/ /pubmed/33322249 http://dx.doi.org/10.3390/molecules25245847 Text en © 2020 by the authors. Licensee MDPI, Basel, Switzerland. This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution (CC BY) license (http://creativecommons.org/licenses/by/4.0/).
spellingShingle Article
Gujarathi, Satheesh
Zafar, Maroof Khan
Liu, Xingui
Eoff, Robert L.
Zheng, Guangrong
A Facile Semisynthesis and Evaluation of Garcinoic Acid and Its Analogs for the Inhibition of Human DNA Polymerase β
title A Facile Semisynthesis and Evaluation of Garcinoic Acid and Its Analogs for the Inhibition of Human DNA Polymerase β
title_full A Facile Semisynthesis and Evaluation of Garcinoic Acid and Its Analogs for the Inhibition of Human DNA Polymerase β
title_fullStr A Facile Semisynthesis and Evaluation of Garcinoic Acid and Its Analogs for the Inhibition of Human DNA Polymerase β
title_full_unstemmed A Facile Semisynthesis and Evaluation of Garcinoic Acid and Its Analogs for the Inhibition of Human DNA Polymerase β
title_short A Facile Semisynthesis and Evaluation of Garcinoic Acid and Its Analogs for the Inhibition of Human DNA Polymerase β
title_sort facile semisynthesis and evaluation of garcinoic acid and its analogs for the inhibition of human dna polymerase β
topic Article
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7763917/
https://www.ncbi.nlm.nih.gov/pubmed/33322249
http://dx.doi.org/10.3390/molecules25245847
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