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1,2,5-Oxadiazole N-oxide derivatives as potential anti-cancer agents: synthesis and biological evaluation. Part IV.
- Source :
-
European journal of medicinal chemistry [Eur J Med Chem] 2001 Oct; Vol. 36 (10), pp. 771-82. - Publication Year :
- 2001
-
Abstract
- Several new 1,2,5-oxadiazole N-oxide derivatives and some deoxygenated analogues were synthesized to be tested as potential selective hypoxic cell cytotoxins. Compounds prepared were designed in order to gain insight into the mechanism of action of this kind of cytotoxin. Compounds were tested in oxia and hypoxia and they proved to be non-selective. 3-Cyano-N(2)-oxide-4-phenyl-1,2,5-oxadiazole showed the best cytotoxic activity in oxia. The cytotoxicity observed for these derivatives could be explained in terms of the electronic characteristics of the 1,2,5-oxadiazole substituents. Electrochemical and ESR studies were performed on the more cytotoxic derivative.
- Subjects :
- Aerobiosis physiology
Animals
Antineoplastic Agents chemistry
Antineoplastic Agents pharmacology
Cell Hypoxia physiology
Cell Line
Cell Survival drug effects
Clone Cells
Cricetinae
Cytotoxins pharmacology
Structure-Activity Relationship
Antineoplastic Agents chemical synthesis
Oxadiazoles chemical synthesis
Oxadiazoles chemistry
Subjects
Details
- Language :
- English
- ISSN :
- 0223-5234
- Volume :
- 36
- Issue :
- 10
- Database :
- MEDLINE
- Journal :
- European journal of medicinal chemistry
- Publication Type :
- Academic Journal
- Accession number :
- 11738485
- Full Text :
- https://doi.org/10.1016/s0223-5234(01)01265-x