title: Diethylenetriamine pentaacetic acid derivative of toremifene and in vitro evaluation in human breast cancer cell line MCF-7.
abstract: Cytotoxic and apoptotic effects of toremifene-diethylenetriamine pentaacetic acid (TOR-DTPA), formed by conjugation of TOR and DTPA, on the MCF-7 cell line were evaluated. TOR-DTPA was synthesized and qualified via gas chromatography-mass spectrometry system, thin layer chromatography, and high performance liquid chromatography methods. To screen the biological properties of TOR-DTPA at determined concentrations, our ongoing effort was to evaluate apoptotic and cytotoxic effects on the MCF-7 cell line. Trypan blue dye exclusion test, XTT, ELISA, and TUNEL assays were utilized to evaluate cytotoxicity and apoptosis. TOR-DTPA has no cytotoxic and limited apoptotic effect on the MCF-7 cell line according to the results of in vitro studies. It is concluded that the lack of obvious apoptotic and cytotoxic effects allows the already proposed ligand, TOR-DTPA, to be improved as a novel hydrophilic ligand for breast imaging.
authors.affiliation: Department of Nuclear Applications, Institute of Nuclear Sciences, Ege University, Izmir, Turkey. ayfer.yurt.kilcar@ege.edu.tr
authors.forename: Ayfer Yurt
authors.initials: AY
authors.lastname: Kilcar
authors.forename: F Zumrut
authors.initials: FZ
authors.lastname: Biber Muftuler
authors.forename: Perihan
authors.initials: P
authors.lastname: Unak
authors.forename: Cigir Biray
authors.initials: CB
authors.lastname: Avci
authors.forename: Cumhur
authors.initials: C
authors.lastname: Gunduz
mesh_terms: D001943:Breast Neoplasms / Q000188:drug therapy*; D045744:Cell Line, Tumor; D004354:Drug Screening Assays, Antitumor; D004797:Enzyme-Linked Immunosorbent Assay; D005260:Female; D008401:Gas Chromatography-Mass Spectrometry; D006801:Humans; D008024:Ligands; D004369:Pentetic Acid / Q000009:adverse effects / Q000031:analogs & derivatives* / Q000737:chemistry / Q000494:pharmacology*; D020845:Selective Estrogen Receptor Modulators / Q000009:adverse effects / Q000737:chemistry / Q000494:pharmacology*; D017312:Toremifene / Q000009:adverse effects / Q000031:analogs & derivatives* / Q000737:chemistry / Q000494:pharmacology*
chemical_list: D008024:Ligands; D020845:Selective Estrogen Receptor Modulators; D004369:Pentetic Acid; D017312:Toremifene