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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MDPI AG
2014-10-01
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| Series: | Marine Drugs |
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| Online Access: | http://www.mdpi.com/1660-3397/12/10/5209 |
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doaj-6a8ebc29db2b475295478b6bbec1e5e22020-11-25T00:01:23ZengMDPI AGMarine Drugs1660-33972014-10-0112105209522110.3390/md12105209md12105209Modification of Marine Natural Product Ningalin B and SAR Study Lead to Potent P-Glycoprotein InhibitorsChao Yang0Iris L. K. Wong1Wen Bin Jin2Tao Jiang3Larry M. C. Chow4Sheng Biao Wan5Key Laboratory of Marine Drugs, Ministry of Education, Shandong Provincial Key Laboratory of Glycoscience & Glycotechnology, School of Medicine and Pharmacy, Ocean University of China, Qingdao 266003, ChinaDepartment of Applied Biology and Chemical Technology, The Hong Kong Polytechnic University, Hung Hom, Hong Kong, ChinaKey Laboratory of Marine Drugs, Ministry of Education, Shandong Provincial Key Laboratory of Glycoscience & Glycotechnology, School of Medicine and Pharmacy, Ocean University of China, Qingdao 266003, ChinaKey Laboratory of Marine Drugs, Ministry of Education, Shandong Provincial Key Laboratory of Glycoscience & Glycotechnology, School of Medicine and Pharmacy, Ocean University of China, Qingdao 266003, ChinaDepartment of Applied Biology and Chemical Technology, The Hong Kong Polytechnic University, Hung Hom, Hong Kong, ChinaKey Laboratory of Marine Drugs, Ministry of Education, Shandong Provincial Key Laboratory of Glycoscience & Glycotechnology, School of Medicine and Pharmacy, Ocean University of China, Qingdao 266003, ChinaIn 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.http://www.mdpi.com/1660-3397/12/10/5209ningalin B analoguesmultidrug resistance (MDR)pyrroleP-glycoproteinP-gp modulators |
| collection |
DOAJ |
| language |
English |
| format |
Article |
| sources |
DOAJ |
| author |
Chao Yang Iris L. K. Wong Wen Bin Jin Tao Jiang Larry M. C. Chow Sheng Biao Wan |
| spellingShingle |
Chao Yang Iris L. K. Wong Wen Bin Jin Tao Jiang Larry M. C. Chow Sheng Biao Wan Modification of Marine Natural Product Ningalin B and SAR Study Lead to Potent P-Glycoprotein Inhibitors Marine Drugs ningalin B analogues multidrug resistance (MDR) pyrrole P-glycoprotein P-gp modulators |
| author_facet |
Chao Yang Iris L. K. Wong Wen Bin Jin Tao Jiang Larry M. C. Chow Sheng Biao Wan |
| author_sort |
Chao Yang |
| title |
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_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_sort |
modification of marine natural product ningalin b and sar study lead to potent p-glycoprotein inhibitors |
| publisher |
MDPI AG |
| series |
Marine Drugs |
| issn |
1660-3397 |
| publishDate |
2014-10-01 |
| 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. |
| topic |
ningalin B analogues multidrug resistance (MDR) pyrrole P-glycoprotein P-gp modulators |
| url |
http://www.mdpi.com/1660-3397/12/10/5209 |
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