title: Modification of marine natural product ningalin B and SAR study lead to potent P-glycoprotein inhibitors.
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.
authors.affiliation: 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. yangchao.hy@163.com.
authors.forename: Chao
authors.initials: C
authors.lastname: Yang
authors.affiliation: Department of Applied Biology and Chemical Technology, The Hong Kong Polytechnic University, Hung Hom, Hong Kong, China. iris.l.k.wong@polyu.edu.hk.
authors.forename: Iris L K
authors.initials: IL
authors.lastname: Wong
authors.affiliation: 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. wenbinjin0418@gmail.com.
authors.forename: Wen Bin
authors.initials: WB
authors.lastname: Jin
authors.affiliation: 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. jiangtao@ouc.edu.cn.
authors.forename: Tao
authors.initials: T
authors.lastname: Jiang
authors.affiliation: Department of Applied Biology and Chemical Technology, The Hong Kong Polytechnic University, Hung Hom, Hong Kong, China. iris.l.k.wong@polyu.edu.hk.
authors.forename: Larry M C
authors.initials: LM
authors.lastname: Chow
authors.affiliation: 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. biaowan@ouc.edu.cn.
authors.forename: Sheng Biao
authors.initials: SB
authors.lastname: Wan
mesh_terms: D020168:ATP Binding Cassette Transporter, Subfamily B, Member 1 / Q000037:antagonists & inhibitors*; D000970:Antineoplastic Agents / Q000737:chemistry / Q000494:pharmacology; D001688:Biological Products / Q000737:chemistry* / Q000494:pharmacology*; D001943:Breast Neoplasms / Q000188:drug therapy; D045744:Cell Line, Tumor; D018432:Drug Resistance, Multiple / Q000187:drug effects; D019008:Drug Resistance, Neoplasm / Q000187:drug effects; D005260:Female; D006575:Heterocyclic Compounds, 3-Ring / Q000737:chemistry* / Q000494:pharmacology*; D006801:Humans; D020014:K562 Cells; D007938:Leukemia / Q000188:drug therapy; D000077489:Piperazine; D010879:Piperazines / Q000737:chemistry / Q000494:pharmacology; D013329:Structure-Activity Relationship
chemical_list: D020168:ATP Binding Cassette Transporter, Subfamily B, Member 1; D000970:Antineoplastic Agents; D001688:Biological Products; D006575:Heterocyclic Compounds, 3-Ring; D010879:Piperazines; C409782:ningalin B; D000077489:Piperazine