The cytotoxicity of trifluoromethyl boron derivatives and mode of action in human Tmolt3 T leukemic cells

✍ Scribed by Iris H. Hall; Jennifer R. Henry; Nathanael J. Peaty; Betsy Jo Barnes; G. Pawelke

• Publisher: John Wiley and Sons
• Year: 2000
• Tongue: English
• Weight: 99 KB
• Volume: 14
• Category: Article
• ISSN: 0268-2605
• DOI: 10.1002/(sici)1099-0739(200002)14:2<86::aid-aoc957>3.0.co;2-y

✦ Synopsis

Trifluoromethylboron derivatives proved to be cytotoxic in a number of murine and human leukemic and lymphoma screens. Solid tumor growth, e.g. glioma HS 683, breast Mck-7 and colon adenocarcinoma SW480, was reduced significantly by the compounds. Human Tmolt 3 T-cell leukemia DNA synthesis was inhibited preferentially by the derivatives, with marginal effects on RNA and protein syntheses, after 60 min at 100 mM. The agents appeared to act by multiple mechanisms in that they inhibited the activities of DNA polymerase a, dihydrofolate reductase and nucleosides, significantly within 60 min at 100 mM. Deoxyribonucleotide pools were reduced after 60 min incubation with the compounds. Tmolt 3 DNA fragmentation and reduced ct-DNA viscosity were evident after 24 h of incubation at 100 mM. ct-DNA thermal denaturation studies indicated that the agents caused some type of interaction with the bases of DNA.