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Mar. Drugs 2014, 12(10), 5209-5221; doi:10.3390/md12105209

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

1
Key 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, China
2
Department of Applied Biology and Chemical Technology, The Hong Kong Polytechnic University, Hung Hom, Hong Kong, China
These authors contributed equally to this work.
*
Author to whom correspondence should be addressed.
Received: 11 March 2014 / Revised: 1 September 2014 / Accepted: 25 September 2014 / Published: 17 October 2014
(This article belongs to the Special Issue Alkaloid Analogs)
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Abstract

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. View Full-Text
Keywords: ningalin B analogues; multidrug resistance (MDR); pyrrole; P-glycoprotein; P-gp modulators ningalin B analogues; multidrug resistance (MDR); pyrrole; P-glycoprotein; P-gp modulators
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This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited. (CC BY 4.0).

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MDPI and ACS Style

Yang, C.; Wong, I.L.K.; Jin, W.B.; Jiang, T.; Chow, L.M.C.; Wan, S.B. Modification of Marine Natural Product Ningalin B and SAR Study Lead to Potent P-Glycoprotein Inhibitors. Mar. Drugs 2014, 12, 5209-5221.

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