Synthesis and Cytotoxic Action of 1‐Oxoalkyl and 1,2‐Dioxoalkyl‐1,2,4‐triazolidine‐3,5‐diones in Murine and Human Tissue Cultured Cells

doi:10.1002/(SICI)1521-4184(19997)332:7<225::AID-ARDP225>3.0.CO;2-2

Paper

Synthesis and Cytotoxic Action of 1‐Oxoalkyl and 1,2‐Dioxoalkyl‐1,2,4‐triazolidine‐3,5‐diones in Murine and Human Tissue Cultured Cells

Published Jul 1, 1999 · DOI · Christopher MacLauchlin, I. Hall, R. Izydore

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Abstract

1‐Oxoalkyl and 1,2‐dioxoalkyl‐1,2,4‐triazolidine‐3,5‐diones proved to be potent antineoplastic agents in mouse tumors and potent cytotoxic agents particularly against the growth of suspended tumor cells. The compounds with shorter substituents in position 1 or positions 1 and 2 afforded the better activity. In L1210 lymphoid leukemia cells DNA, RNA, and protein syntheses were inhibited at 100 μM after 60 min. Multiple enzyme sites in nucleic acid metabolism were affected by the compounds, i.e. DNA polymerase α, PRPP‐amido transferase, dihydrofolate reductase, thymidylate synthetase, and nucleoside kinases. These effects of the agents are probably additive in bringing about inhibition of DNA synthesis and cell death.

In Vitro Study

Study Snapshot

1Oxoalkyl and 1,2Dioxoalkyl1,2,4triazolidine3,5diones show potent antineoplastic and cytotoxic effects against tumor growth, with shorter substituents in positions 1 and 2 offering better activity.

PopulationOlder adults (50-71 years)

Sample size24

MethodsObservational

OutcomesBody Mass Index projections

ResultsSocial networks mitigate obesity in older groups.

Synthesis and Cytotoxic Action of 1‐Oxoalkyl and 1,2‐Dioxoalkyl‐1,2,4‐triazolidine‐3,5‐diones in Murine and Human Tissue Cultured Cells

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