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Open AccessArticle

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
*
Author to whom correspondence should be addressed.
These authors contributed equally to this work.
Mar. Drugs 2014, 12(10), 5209-5221; https://doi.org/10.3390/md12105209
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)
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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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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