Modification of Marine Natural Product Ningalin B and SAR Study Lead to Potent P-Glycoprotein Inhibitors

In this study, new marine ningalin B analogues containing a piperazine or a benzoloxy group at ring C have been synthesized and evaluated on their P-gp modulating activity in human breast cancer and leukemia cell lines. Their structure-activity relationship was preliminarily studied. Compounds 19 an...

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Autores principales: Yang, Chao, Wong, Iris L. K., Jin, Wen Bin, Jiang, Tao, Chow, Larry M. C., Wan, Sheng Biao
Formato: Online Artículo Texto
Lenguaje:English
Publicado: MDPI 2014
Materias:
Article
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4210895/
https://www.ncbi.nlm.nih.gov/pubmed/25329704
http://dx.doi.org/10.3390/md12105209
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author Yang, Chao
Wong, Iris L. K.
Jin, Wen Bin
Jiang, Tao
Chow, Larry M. C.
Wan, Sheng Biao
author_facet Yang, Chao
Wong, Iris L. K.
Jin, Wen Bin
Jiang, Tao
Chow, Larry M. C.
Wan, Sheng Biao
author_sort Yang, Chao
collection PubMed
description In this study, new marine ningalin B analogues containing a piperazine or a benzoloxy group at ring C have been synthesized and evaluated on their P-gp modulating activity in human breast cancer and leukemia cell lines. Their structure-activity relationship was preliminarily studied. Compounds 19 and 20 are potent P-gp inhibitors. These two synthetic analogues of permethyl ningalin B may be potentially used as effective modulators of P-gp-mediated drug resistance in cancer cells.
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spelling pubmed-42108952014-10-28 Modification of Marine Natural Product Ningalin B and SAR Study Lead to Potent P-Glycoprotein Inhibitors Yang, Chao Wong, Iris L. K. Jin, Wen Bin Jiang, Tao Chow, Larry M. C. Wan, Sheng Biao Mar Drugs Article In this study, new marine ningalin B analogues containing a piperazine or a benzoloxy group at ring C have been synthesized and evaluated on their P-gp modulating activity in human breast cancer and leukemia cell lines. Their structure-activity relationship was preliminarily studied. Compounds 19 and 20 are potent P-gp inhibitors. These two synthetic analogues of permethyl ningalin B may be potentially used as effective modulators of P-gp-mediated drug resistance in cancer cells. MDPI 2014-10-17 /pmc/articles/PMC4210895/ /pubmed/25329704 http://dx.doi.org/10.3390/md12105209 Text en © 2014 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 license (http://creativecommons.org/licenses/by/4.0/).
spellingShingle Article
Yang, Chao
Wong, Iris L. K.
Jin, Wen Bin
Jiang, Tao
Chow, Larry M. C.
Wan, Sheng Biao
Modification of Marine Natural Product Ningalin B and SAR Study Lead to Potent P-Glycoprotein Inhibitors
title Modification of Marine Natural Product Ningalin B and SAR Study Lead to Potent P-Glycoprotein Inhibitors
title_full Modification of Marine Natural Product Ningalin B and SAR Study Lead to Potent P-Glycoprotein Inhibitors
title_fullStr Modification of Marine Natural Product Ningalin B and SAR Study Lead to Potent P-Glycoprotein Inhibitors
title_full_unstemmed Modification of Marine Natural Product Ningalin B and SAR Study Lead to Potent P-Glycoprotein Inhibitors
title_short Modification of Marine Natural Product Ningalin B and SAR Study Lead to Potent P-Glycoprotein Inhibitors
title_sort modification of marine natural product ningalin b and sar study lead to potent p-glycoprotein inhibitors
topic Article
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4210895/
https://www.ncbi.nlm.nih.gov/pubmed/25329704
http://dx.doi.org/10.3390/md12105209
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