Abstract |
A series of synthetic chalcones, flavanones, and flavones has been synthesized and evaluated for antitumor activity against the human kidney carcinoma cells TK-10, human mammary adenocarcinoma cells MCF-7 ( estrogen receptor-positive), and human colon adenocarcinoma cells HT-29. The most active series is the chalcone ones with the best results against TK-10 and HT-29 cells. Fourteen out of 53 analyzed compounds resulted very active against at least two of the studied tumoral cells. Alkaline single cell gel electrophoresis, comet assay, was performed as a study of the chromosomal aberrations promoted by the compounds on normal cells. Four active and two inactive chalcones were studied in the comet assay against normal human kidney cells (HK-2). A structure-activity relationship analysis of these compounds was performed and for 4- and 3,4-disubstituted derivatives a quantitative correlation was obtained in the case of anti-HT-29 activity.
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Authors | Mauricio Cabrera, Macarena Simoens, Gabriela Falchi, M Laura Lavaggi, Oscar E Piro, Eduardo E Castellano, Anabel Vidal, Amaia Azqueta, Antonio Monge, Adela López de Ceráin, Gabriel Sagrera, Gustavo Seoane, Hugo Cerecetto, Mercedes González |
Journal | Bioorganic & medicinal chemistry
(Bioorg Med Chem)
Vol. 15
Issue 10
Pg. 3356-67
(May 15 2007)
ISSN: 0968-0896 [Print] England |
PMID | 17383189
(Publication Type: Journal Article, Research Support, Non-U.S. Gov't)
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Chemical References |
- Antineoplastic Agents
- Chalcones
- DNA, Neoplasm
- Flavones
- Indicators and Reagents
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Topics |
- Antineoplastic Agents
(chemical synthesis, pharmacology)
- Cell Line, Tumor
- Chalcones
(chemical synthesis, pharmacology)
- Chromatography, Thin Layer
- Chromosome Aberrations
(drug effects)
- Comet Assay
- DNA Damage
- DNA, Neoplasm
(drug effects)
- Drug Screening Assays, Antitumor
- Flavones
(chemical synthesis, pharmacology)
- Humans
- Indicators and Reagents
- Magnetic Resonance Spectroscopy
- Mass Spectrometry
- Spectrophotometry, Infrared
- Structure-Activity Relationship
- X-Ray Diffraction
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