Synthesis, anticancer activities and molecular modeling studies of novel indole retinoid derivatives
Selen Gurkan-Alp, A.
European Journal of Medicinal Chemistry
346 - 354
MetadataShow full item record
Please cite this item using this persistent URLhttp://hdl.handle.net/11693/21191
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 IC50 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. © 2012 Elsevier Masson SAS. All rights reserved.
Showing items related by title, author, creator and subject.
Retinoid N-(1H-benzo[d]imidazol-2-yl)-5,5,8,8-tetramethyl-5,6,7,8-tetrahydronaphthalene-2-carboxamide induces p21-dependent senescence in breast cancer cells Mumcuoglu M.; Gurkan-Alp A.S.; Buyukbingol E.; Cetin-Atalay R. (Elsevier Inc., 2016)Retinoids have been implicated as pharmacological agents for the prevention and treatment of various types of cancers, including breast cancers. We analyzed 27 newly synthesized retinoids for their bioactivity on breast, ...
Synthesis, anticancer activities and molecular modeling studies of novel indole retinoid derivatives Gurkan Alp, A. S.; Mumcuoglu, M.; Andac, C. A.; Dayanc, E.; Cetin Atalay, R.; Buyukbingol, E. (Elsevier, 2012-10)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. ...
Synthesis and cytotoxic activity of novel 3-methyl-1-[(4- substitutedpiperazin-1-yl)methyl]-1H-indole derivatives Koksal, M.; Yarim, M.; Durmaz I.; Cetin-Atalay, R. (2012)A series of novel 3-methyl-1-[(4-substitutedpiperazin-1-yl)methyl]-1H- indoles (3a-l) were synthesized and their cytotoxicities were analyzed against 3 different human cell lines, including liver (HUH7), breast (MCF7) and ...