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Modification of Marine Natural Product Ningalin B and SAR Study Lead to Potent P-Glycoprotein Inhibitors |
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| Authors: | Chao Yang Iris L. K. Wong Wen Bin Jin Tao Jiang Larry M. C. Chow Sheng Biao Wan |
| Affiliation: | 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; E-Mails: (C.Y.); (W.B.J.); (T.J.);2.Department of Applied Biology and Chemical Technology, The Hong Kong Polytechnic University, Hung Hom, Hong Kong, China; E-Mail: |
| 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. |
| Keywords: | ningalin B analogues multidrug resistance (MDR) pyrrole P-glycoprotein P-gp modulators |