Synthetic chalcones, flavanones, and flavones as antitumoral agents: biological evaluation and structure-activity relationships.
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| 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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