title: Synthesis of 2-methyl N10-substituted acridones as selective inhibitors of multidrug resistance (MDR) associated protein in cancer cells.
abstract: A series of N10-substituted-2-methyl acridone derivatives are synthesized and are examined for its ability to reverse P-glycoprotein (P-gp) mediated multidrug resistance (MDR) in breast cancer cell lines MCF-7 and MCF-7/Adr. The structural requirement of in-vitro anti-cancer and reversal of drug resistance are studied. The results showed that compound 16 with four carbon spacer exhibited promising in-vitro anti-cancer and reversal of drug resistance in comparison to the other analogues.
authors.affiliation: Department of Medical Oncology, Cancer Center Amsterdam, VU Medical Center, Amsterdam, The Netherlands. mayuryc@rediffmail.com
authors.forename: Y C
authors.initials: YC
authors.lastname: Mayur
authors.forename: Osman
authors.initials: O
authors.lastname: Ahmad
authors.forename: V V S Rajendra
authors.initials: VV
authors.lastname: Prasad
authors.forename: M N
authors.initials: MN
authors.lastname: Purohit
authors.forename: N
authors.initials: N
authors.lastname: Srinivasulu
authors.forename: S M Shanta
authors.initials: SM
authors.lastname: Kumar
mesh_terms: D020168:ATP Binding Cassette Transporter, Subfamily B, Member 1 / Q000378:metabolism; D054831:Acridones / Q000138:chemical synthesis / Q000494:pharmacology*; D000970:Antineoplastic Agents / Q000138:chemical synthesis / Q000494:pharmacology*; D001943:Breast Neoplasms / Q000378:metabolism / Q000473:pathology; D045744:Cell Line, Tumor / Q000187:drug effects / Q000473:pathology; D019008:Drug Resistance, Neoplasm; D006801:Humans; D008956:Models, Chemical; D027425:ATP-Binding Cassette, Sub-Family C Proteins / Q000037:antagonists & inhibitors*
chemical_list: D020168:ATP Binding Cassette Transporter, Subfamily B, Member 1; D054831:Acridones; D000970:Antineoplastic Agents; D027425:ATP-Binding Cassette, Sub-Family C Proteins