Synthetic chalcones, flavanones, and flavones as antitumoral agents: Biological evaluation and structure–activity relationships
A wide series of synthetic flavonoids, with druglikeness properties, were developed and evaluated as antitumoral agents against TK-10, MCF-7, and HT-29 human tumoral cells. Comet assay was performed against non-tumoral HK-2 in order to know chromosomal aberrations in normal cells. A QSAR was obtaine...
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Published in | Bioorganic & medicinal chemistry Vol. 15; no. 10; pp. 3356 - 3367 |
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Main Authors | , , , , , , , , , , , , , |
Format | Journal Article |
Language | English |
Published |
Oxford
Elsevier Ltd
15.05.2007
Elsevier Science |
Subjects | |
Online Access | Get full text |
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Summary: | A wide series of synthetic flavonoids, with druglikeness properties, were developed and evaluated as antitumoral agents against TK-10, MCF-7, and HT-29 human tumoral cells. Comet assay was performed against non-tumoral HK-2 in order to know chromosomal aberrations in normal cells. A QSAR was obtained for anti-HT-29 activities.
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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ISSN: | 0968-0896 1464-3391 |
DOI: | 10.1016/j.bmc.2007.03.031 |