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

Marine Drugs

Chao Yang¹  Iris L. K. Wong²  Wen Bin Jin¹  Tao Jiang¹  Larry M. C. Chow²  Sheng Biao Wan¹ 

[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:;Department of Applied Biology and Chemical Technology, The Hong Kong Polytechnic University, Hung Hom, Hong Kong, China; E-Mail:

关键词: ningalin B analogues;    multidrug resistance (MDR);    pyrrole;    P-glycoprotein;    P-gp modulators;   

DOI  :  10.3390/md12105209

来源: mdpi

【 摘 要 】

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.

【 授权许可】

CC BY   
© 2014 by the authors; licensee MDPI, Basel, Switzerland.