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首页> 外文期刊>Acta Biochimica Polonica >Synthesis of kaempferide Mannich base derivatives and their antiproliferative activity on three human cancer cell lines
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Synthesis of kaempferide Mannich base derivatives and their antiproliferative activity on three human cancer cell lines

机译：Kaempferide曼尼希碱衍生物的合成及其对三种人类癌细胞系的抗增殖活性

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摘要

Kaempferide (3,5,7-trihydroxy-4'-methoxyflavone, 1), a naturally occurring flavonoid with potent anticancer activity in a number of human tumour cell lines, was first semisynthesized from naringin. Based on Mannich reaction of kaempferide with various secondary amines and formaldehyde, nine novel kaempferide Mannich base derivatives 2-10 were synthesized. The aminomethylation occurred preferentially in the position at C-6 and C-8 of the A-ring of kaempferide. All the synthetic compounds were tested for antiproliferative activity against three human cancer cell lines (Hela, HCC1954, SK-OV-3) by the standard MTT method. The results showed that compounds 1, 2 and 5-10 were more potent against Hela cells with IC50 values of 12.47-28.24 mu M than the positive control cis-platin (IC50 41.25 mu M), compounds 5, 6, 8 and 10 were more potent against HCC1954 cells with IC50 values of 8.82-14.97 mu M than the positive control cis-platin (IC50 29.68 mu M), and compounds 2, 3, 5, 6 and 10 were more potent against SK-OV-3 cells with IC50 values of 7.67-18.50 mu M than the positive control cis-platin (IC50 21.27 mu M).
机译：Kaempferide（3,5,7-三羟基-4'-甲氧基黄酮，1）是天然存在的类黄酮，在许多人类肿瘤细胞系中具有强大的抗癌活性，首先是由柚皮苷半合成的。基于Kaempferide与各种仲胺和甲醛的Mannich反应，合成了九种新型Kaempferide Mannich碱衍生物2-10。氨基甲基化优先发生在山emp素A环的C-6和C-8位置。通过标准MTT方法测试所有合成化合物对三种人类癌细胞系（Hela，HCC1954，SK-OV-3）的抗增殖活性。结果表明，化合物1、2和5-10对Hela细胞的效价比阳性对照顺铂（IC50 41.25μM）强，IC50值为12.47-28.24μM，化合物5、6、8和10为对HCC1954细胞的IC50值比阳性对照顺铂（IC50 29.68μM）更强，化合物2、3、5、6和10对SK-OV-3细胞更有效。 IC50值比阳性对照顺铂（IC50 21.27μM）高7.67-18.50μM。

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