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首页> 外文期刊>Natural product communications >Facile synthesis of chrysin-derivatives with promising activities as aromatase inhibitors.
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Facile synthesis of chrysin-derivatives with promising activities as aromatase inhibitors.

机译：容易合成具有希望的芳香酶抑制剂活性的菊花素衍生物。

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摘要

Flavones such as chrysin show structural similarities to androgens, the substrates of human aromatase, which converts androgens to estrogens. Aromatase is a key target in the treatment of hormone-dependent tumors, including breast cancer. Flavone-based aromatase inhibitors are of growing interest, and chrysin in particular provides a (natural) lead structure. This paper reports multicomponent synthesis as a means for facile modification of the chrysin core structure in order to add functional elements. A Mannich-type reaction was used to synthesize a range of mono- and disubstituted chrysin derivatives, some of which are more effective aromatase inhibitors than the benchmark compound, aminoglutethimide. Similarly, the reaction of chrysin with various isonitriles and acetylene dicarboxylates results in a new class of flavone derivatives, tricyclic pyrano-flavones which also inhibit human aromatase. Multicomponent reactions involving flavones therefore enable the synthesis of a variety of derivatives, some of which may be useful as anticancer agents.
机译：类黄酮（如菊花蛋白）与雄激素（人类芳香酶的底物）具有结构相似性，后者将雄激素转化为雌激素。芳香酶是治疗激素依赖性肿瘤（包括乳腺癌）的关键靶标。基于黄酮的芳香化酶抑制剂的兴趣日益增长，尤其是菊花链素提供了一种（天然的）铅结构。本文报道了多组分合成方法，该方法可方便地修饰菊花链核心结构，以添加功能性元素。使用曼尼希型反应合成了一系列单取代和双取代的菊花素衍生物，其中一些比基准化合物氨基戊二酰亚胺更有效。类似地，菊花素与各种异腈和乙炔二羧酸酯的反应产生了一类新的黄酮衍生物，三环吡喃类黄酮也抑制人的芳香酶。因此，涉及黄酮的多组分反应能够合成多种衍生物，其中一些可用作抗癌剂。

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