Computed Properties of C7H4F2O2. Baecker, D; Obermoser, V; Kirchner, EA; Hupfauf, A; Kircher, B; Gust, R in [Baecker, Daniel; Obermoser, Victoria; Kirchner, Elisabeth Anna; Hupfauf, Andrea; Gust, Ronald] Univ Innsbruck, CCB, CMBI, Inst Pharm,Dept Pharmaceut Chem, A-6020 Innsbruck, Austria; [Kircher, Brigitte] Innsbruck Med Univ, Dept Internal Med Hematol & Oncol 5, Immunobiol & Stem Cell Lab, Anichstr 35, A-6020 Innsbruck, Austria; [Kircher, Brigitte] Tyrolean Canc Res Inst, Innrain 64, A-6020 Innsbruck, Austria published Fluorination as tool to improve bioanalytical sensitivity and COX-2-selective antitumor activity of cobalt alkyne complexes in 2019, Cited 59. The Name is 2,6-Difluorobenzoic acid. Through research, I have a further understanding and discovery of 385-00-2.
The cobalt alkyne complex [(prop-2-ynyl)-2-acetoxybenzoate]dicobalthexacarbonyl (Co-ASS) is an auspicious lead, which exhibits its anticancer activity mainly by inhibition of both cyclooxygenases (COX-1 and COX-2). Since COX-2 participates in carcinogenesis, a selective inhibition of that isoenzyme is aimed. To study if fluorination increases the COX-2/COX-1 inhibition ratio of the lead, substitution was respectively performed in the positions 3, 4, 5, and 6 of the aromatic moiety. The complexes 3/4/5F-Co-ASS and to a much lower extent also 6F-Co-ASS showed cytotoxic, antimetabolic, and apoptotic effects in COX-1/2-positive HT-29 and MDA-MB-231 cells and remarkably less activity in the COX-1/2-negative MCF-7 cell line. The metabolic activity in MCF-7 cells was even unaffected up to a concentration of 40 mu M. With exception of 6F-Co-ASS, the complexes strongly reduced the PGE(2) synthesis in HT-29 cells and all complexes inhibited COX-2 more effectively than COX-1 in an assay at isolated enzymes. These findings point to an interference in the COX cascade as part of the mode of antitumor action. The limited cellular effects of 6F-Co-ASS are related to its poor uptake as determined by HR CS AAS/MAS. Moreover, the cellular uptake studies confirm fluorination as beneficial tool for bioanalytical labeling. The higher quantification of fluorine by HR CS MAS makes this method about 5-fold more sensitive than HR CS AAS measuring cobalt. As a further positive result, 3/4/5/6-Co-ASS demonstrated high selectivity to tumor cells due to lack of antimetabolic activity against the non-tumorigenic bone marrow stromal cell line HS-5.
Computed Properties of C7H4F2O2. Welcome to talk about 385-00-2, If you have any questions, you can contact Baecker, D; Obermoser, V; Kirchner, EA; Hupfauf, A; Kircher, B; Gust, R or send Email.
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