| 靖铮 宋化龙 王汝冰 李绍顺.萘查耳酮类化合物的设计合成及对CYP1B1 酶
的抑制活性评价[J].,2014,14(7):1229-1234 |
| 萘查耳酮类化合物的设计合成及对CYP1B1 酶
的抑制活性评价 |
| Synthesis and CYP1B1 Inhibitory Activity of Benzo-chalcone Derivatives |
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| DOI： |
| 中文关键词: 萘查耳酮 CYP1B1 酶抑制剂 合成 抗肿瘤 |
| 英文关键词: Benzo-chalcone CYP1B1 Synthesis Antitumor |
| 基金项目: |
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| 摘要点击次数: 767 |
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| 中文摘要: |
| 目的：设计并合成几类新型的萘查耳酮衍生物，初步测定其对CYP1B1 酶的抑制活性，筛选具有良好抗癌作用的CYP1B1
抑制剂。方法：以1,5-二羟基萘为原料，首先合成两个重要的中间体2-乙酰基-1, 4, 5, 8- 四甲氧基萘、1, 5, 6- 三甲氧基-2- 萘乙
酮，然后利用羟醛缩合反应合成所需要的化合物。结果：合成了19 个目标化合物，其结构均经过核磁共振氢谱确证，所有化合物
均为全新化合物。对所合成的新化合物均进行了EROD酶实验测定。结论：所合成的化合物均具有较强的CYP1B1 酶一抑制活
性，其中4-1、4-2、5'-1 对CYP1B1 的抑制活性强于CYP1B1 强抑制剂alpha- 萘黄酮（IC50=11 nmol/L），他们的IC50分别为6.5、0.47、8
nmol/L。 |
| 英文摘要: |
| Objective:A series of benzo-chalcone derivatives were designed and synthesized, and then they were tested for their CYP1B1
inhibitory activities to find some potent CYP1B1 inhibitors which might have good anticancer effects.Methods:1, 5-dihydroxynaphthalene
was used as the starting material, then two important intermediates (2-acetyl-1, 4, 5, 8-tetramethoxy-naphthalene and 1, 5, 6-
trimethoxy-2-acetonaphthone) were synthesized. Finally, target compounds were synthesized through aldol reaction. Results:Nineteen
novel benzo-chalcone derivatives were synthesized, and their structures were confirmed by 1H-NMR. Moreover, their enzyme inhibitory
activities were also tested through enzyme assay.Conclusion:The CYP1B1 inhibitory activities of the target compounds were evaluated
and the results demonstrated that most of themhad potent inhibition against CYP1B1. Among all these compounds, 4-1, 4-2and 5'-1 were
the most potent CYP1B1 inhibitors with the IC50 value of 6.5, 0.47, 8 nmol/L, which even better than alpha-naphthoflavone (IC50=11 nmol/L). |
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