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Potential antitumor agents. 37. Synthesis and antitumor activity of guanylhydrazones from imidazo[2,1-b]thiazoles and from the new heterocyclic system thiazolo[2',3':2,3]imidazo[4,5-c]quinoline.
- Source :
-
Journal of medicinal chemistry [J Med Chem] 2005 Apr 21; Vol. 48 (8), pp. 3085-9. - Publication Year :
- 2005
-
Abstract
- This paper reports synthesis and antitumor activity of new guanylhydrazones from imidazo[2,1-b]thiazoles and from the new heterocyclic system thiazolo[2',3':2,3]imidazo[4,5-c]quinoline. The compounds were tested as potential antitumor agents at the National Cancer Institute. The effect of the guanylhydrazone of 2-chloro-6-(2,5-dimethoxy-4-nitrophenyl)imidazo[2,1-b]thiazole-5-carbaldehyde (41) was investigated, and it was found to be an inhibitor of Complex III of the mitochondrial respiratory chain and is able to induce apoptosis in the cell lines HT29 and HL60.
- Subjects :
- Animals
Antineoplastic Agents chemistry
Antineoplastic Agents pharmacology
Cell Line, Tumor
Cell Proliferation drug effects
Cell Survival drug effects
Drug Screening Assays, Antitumor
Humans
Hydrazones chemistry
Hydrazones pharmacology
Imidazoles chemistry
Imidazoles pharmacology
In Vitro Techniques
Membrane Potentials drug effects
Mitochondria, Liver drug effects
Mitochondria, Liver metabolism
Oxygen Consumption drug effects
Quinolines chemistry
Quinolines pharmacology
Rats
Structure-Activity Relationship
Thiazoles chemistry
Thiazoles pharmacology
Antineoplastic Agents chemical synthesis
Hydrazones chemical synthesis
Imidazoles chemical synthesis
Quinolines chemical synthesis
Thiazoles chemical synthesis
Subjects
Details
- Language :
- English
- ISSN :
- 0022-2623
- Volume :
- 48
- Issue :
- 8
- Database :
- MEDLINE
- Journal :
- Journal of medicinal chemistry
- Publication Type :
- Academic Journal
- Accession number :
- 15828848
- Full Text :
- https://doi.org/10.1021/jm040888s