Synthesis and Cytotoxic Action of 3,5‐Isoxazolidinediones and 2‐Isoxazolin‐5‐ones in Murine and Human Tumors

doi:10.1002/ardp.19973300306

Paper

Synthesis and Cytotoxic Action of 3,5‐Isoxazolidinediones and 2‐Isoxazolin‐5‐ones in Murine and Human Tumors

Published 1997 · I. Hall, R. Izydore, Xaioming Zhou

Archiv der Pharmazie

Q2 SJR score

11

Citations

0

Influential Citations

Full textSemantic Scholar

Abstract

The 3,5‐isoxazolidinediones and 2‐isoxazolin‐5‐ones demonstrated potent cytotoxicity against the growth of human Tmolt3 T cell leukemia, murine P388 and L1210 leukemias, as well as human HeLa‐S3 uterine carcinoma and glioma tumor cell growth. The specificity of the 3,5‐isoxazolidinedione and 2‐isoxazoline‐5‐one derivatives as cytotoxic agents varied with the histological type of tumor cell. Selected compounds were active against solid HeLa uterine, KB nasopharynx, skin A431, SW‐480 adenocarcinoma, osteosarcoma and glioma growth. Selected compounds demonstrated in vivo antineoplastic activity against Ehrlich ascites carcinoma growth. In L‐1210 leukemia cells, the agents blocked DNA and protein synthesis at 25,50 and 100 μM over 60 min. The agents were effective in reducing rate limiting enzymes in the de novo purine and pyrimidine pathways. In addition they suppressed dihydrofolate reductase and ribonucleoside reductase activities with moderate inhibition of DNA and RNA polymerase activities. DNA itself was not a target of the agents.

In Vitro Study

Study Snapshot

3,5-isoxazolidinediones and 2-isoxazoline-5-ones show potent cytotoxicity against various human and murine tumors, with specificity varying by tumor type.

PopulationOlder adults (50-71 years)

Sample size24

MethodsObservational

OutcomesBody Mass Index projections

ResultsSocial networks mitigate obesity in older groups.

Paper

Synthesis and Cytotoxic Action of 3,5‐Isoxazolidinediones and 2‐Isoxazolin‐5‐ones in Murine and Human Tumors

References

Structure and Conformations of Monoacyl and Diacyl 1,2,4-Triazolidine-3,5-diones.

Monoacyl and diacyl 1,2,4-triazolidine-3,5-diones with phenyl or tert-butyl groups show acylation on nitrogen, and their structures and conformations can be assigned using NMR spectroscopy and molecular modeling.

Hypolipidemic activity of 4-substituted 1,2-diacyl-1,2,4-triazolidine-3,5-diones in rodents.

The 1,2-diacyl-1,2,4-triazolidine-3,5-diones effectively reduce serum cholesterol and triglyceride levels in rodents by inhibiting lipid synthesis-related enzymes.

Synthesis and hypolipidemic activity of 4-substituted 1-acyl-1,2,4-triazolidine-3,5-diones in rodents.

4-substituted 1-acyl-1,2,4-triazolidine-3,5-diones effectively lower serum cholesterol and triglyceride levels in rodents, suggesting their potential as a new class of cholesterol-lowering drugs.

Reaction of 4,4-diethyl-3,5-pyrazolidinedione with carboxylic acid anhydrides. N-acylation vs O-acylation

15 N NMR spectroscopy is a useful technique for establishing the position(s) of acylation in pyrazolidinedione reactions.

Antimalarial agents. III. Mechanism of action of artesunate against Plasmodium berghei infection.

Artesunate inhibits Plasmodium berghei infection growth by inhibiting DNA synthesis, reducing oxygen consumption, and potentially interfering with cell growth energy requirements.

Citations