title: Partial synthesis and biological evaluation of bisbenzylisoquinoline alkaloids derivatives: potential modulators of multidrug resistance in cancer.
abstract: A series of new bisbenzylisoquinoline alkaloids was partially synthesized from tetrandrine and fangchinoline and evaluated for their ability to reverse P-glycoprotein-mediated multidrug resistance (MDR) in cancer cells. All the test compounds increased the intracellular accumulation rate of rhodamine 123 in MDR cells (Bel7402 and HCT8), and most exhibited more potent MDR-reversing activity relative to the reference compound verapamil. Compounds 8, 10, 13, and 14 enhanced intracellular accumulation of doxorubicin in Bel7402 and HCT8 cells.
authors.affiliation: Department of Chemistry of Medicinal Natural Products, West China College of Pharmacy, Sichuan University, Chengdu 610041, China.
authors.forename: Ping
authors.initials: P
authors.lastname: He
authors.forename: Hua
authors.initials: H
authors.lastname: Sun
authors.forename: Xi-Xian
authors.initials: XX
authors.lastname: Jian
authors.forename: Qiao-Hong
authors.initials: QH
authors.lastname: Chen
authors.forename: Dong-Lin
authors.initials: DL
authors.lastname: Chen
authors.forename: Geng-Tao
authors.initials: GT
authors.lastname: Liu
authors.forename: Feng-Peng
authors.initials: FP
authors.lastname: Wang
mesh_terms: D020168:ATP Binding Cassette Transporter, Subfamily B, Member 1 / Q000187:drug effects; D000470:Alkaloids / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D044182:Benzylisoquinolines / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D004317:Doxorubicin / Q000494:pharmacology; D018432:Drug Resistance, Multiple / Q000187:drug effects*; D006801:Humans; D015394:Molecular Structure; D020112:Rhodamine 123 / Q000032:analysis
chemical_list: D020168:ATP Binding Cassette Transporter, Subfamily B, Member 1; D000470:Alkaloids; D044182:Benzylisoquinolines; D020112:Rhodamine 123; C009438:tetrandrine; D004317:Doxorubicin; C060802:fangchinoline