title: Synthesis, anticancer activities and molecular modeling studies of novel indole retinoid derivatives.
abstract: In this study, novel (E)-3-(5-substituted-1H-indol-3-yl)-1-(5,5,8,8-tetramethyl-5,6,7,8-tetrahydronaphthalen-2-yl)prop-2-en-1-one (5(a-e)) derivatives were synthesized and their anticancer effects were determined in vitro. Novel indole retinoid compounds except 5e have anti-proliferative capacity in liver, breast and colon cancer cell lines. This anti-proliferative effect was further analyzed in breast cancer cell line panel by using the most potent compound 5a. It was determined that 5a can inhibit proliferation at very low IC(50) concentrations in all of the breast cancer cell lines. Here, we present some evidence on apoptotic termination of cancer cell proliferation which may be primarily driven by the inhibition of RXRα and, to a lesser extent, RXRγ.
authors.affiliation: Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Ankara University, Tandogan, Ankara 06100 Turkey. sgurkan@pharmacy.ankara.edu.tr
authors.forename: A Selen
authors.initials: AS
authors.lastname: Gurkan-Alp
authors.forename: Mine
authors.initials: M
authors.lastname: Mumcuoglu
authors.forename: Cenk A
authors.initials: CA
authors.lastname: Andac
authors.forename: Emre
authors.initials: E
authors.lastname: Dayanc
authors.forename: Rengul
authors.initials: R
authors.lastname: Cetin-Atalay
authors.forename: Erdem
authors.initials: E
authors.lastname: Buyukbingol
mesh_terms: D000970:Antineoplastic Agents / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D049109:Cell Proliferation / Q000187:drug effects; D018360:Crystallography, X-Ray; D004305:Dose-Response Relationship, Drug; D004354:Drug Screening Assays, Antitumor; D006801:Humans; D008958:Models, Molecular; D056004:Molecular Dynamics Simulation; D015394:Molecular Structure; D012176:Retinoids / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D013329:Structure-Activity Relationship; D013696:Temperature; D014407:Tumor Cells, Cultured
chemical_list: D000970:Antineoplastic Agents; D012176:Retinoids