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首页> 外文期刊>Bioorganic and Medicinal Chemistry >Synthetic chalcones, flavanones, and flavones as antitumoral agents: Biological evaluation and structure-activity relationships
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Synthetic chalcones, flavanones, and flavones as antitumoral agents: Biological evaluation and structure-activity relationships

机译：合成的查耳酮，黄烷酮和黄酮类药物作为抗肿瘤药：生物学评估和构效关系

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摘要

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.
机译：合成了一系列合成的查耳酮，黄烷酮和黄酮，并评估了其对人肾癌细胞TK-10，人乳腺腺癌细胞MCF-7（雌激素受体阳性）和人结肠腺癌细胞HT-29的抗肿瘤活性。 。最活跃的系列是查耳酮系列，对TK-10和HT-29细胞的效果最佳。在53种分析化合物中，有14种对至少两个研究的肿瘤细胞具有非常高的活性。进行碱性单细胞凝胶电泳彗星试验，以研究化合物在正常细胞上促进的染色体畸变。在彗星试验中研究了针对正常人肾细胞（HK-2）的四个有活性和无活性的查耳酮。进行了这些化合物的结构-活性关系分析，并且对于4-和3,4-二取代的衍生物，在抗HT-29活性的情况下获得了定量相关性。

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