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首页> 外文期刊>RSC Advances >Phosphate tricyclic coumarin analogs as steroid sulfatase inhibitors: synthesis and biological activity
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Phosphate tricyclic coumarin analogs as steroid sulfatase inhibitors: synthesis and biological activity

机译：磷酸三环香豆素类似物作为甾族硫酸酯酶抑制剂：合成和生物活性

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摘要

In the present work, we report convenient methods for the synthesis and biological evaluation of phosphate tricyclic coumarin derivatives as potential steroid sulfatase inhibitors. The described synthesis includes the straightforward preparation of 7-hydroxy-2,3-dihydro-1H-cyclopenta[c]chromen-4-one, 3-hydroxy-7,8,9,10-tetrahydro-6H-benzo[c]chromen-6-one and 3-hydroxy-8,9,10,11-tetrahydro-7H-cyclohepta[c]chromen-6-one modified with various phosphate moieties. The inhibitory effects of the synthesized compounds were tested on STS isolated from human placenta as well as the MCF-7, MDA-MB-231 and MDA-MB-435S cancer cell lines. Most of the new STS inhibitors possessed IC50 values between 21 to 159 mu M. In the course of our investigation, the largest inhibitory effects in the STS enzyme assays were observed for the three compounds 9p, 9r and 9s, with IC50 values of 36.4, 37.8 and 21.5 mu M, respectively (IC50 value of 1.0 mu M for the 665-COUMATE used as a reference). The compound 9r, exhibited the highest potency against MCF-7, an estrogen receptor positive (ER+) cell line, with a GI(50) value of 24.7 mu M. The structure-activity relationships of the synthesized coumarin derivatives with the STS enzyme are discussed.
机译：在本工作中，我们报告了作为潜在的类固醇硫酸酯酶抑制剂的磷酸三环香豆素衍生物的合成和生物学评估的便捷方法。所描述的合成方法包括直接制备7-羟基-2,3-二氢-1H-环戊基[c]铬烯-4-酮，3-羟基-7,8,9,10-四氢-6H-苯并[c] chromen-6-one和3-hydroxy-8,9,10,11-tetrahydro-7H-cyclohepta [c] chromen-6-用各种磷酸酯部分改性。测试了合成化合物对从人胎盘分离的STS以及MCF-7，MDA-MB-231和MDA-MB-435S癌细胞系的抑制作用。大多数新的STS抑制剂的IC50值在21至159μM之间。在我们的研究过程中，STS酶测定法对三种化合物9p，9r和9s的抑制作用最大，IC50值为36.4，分别为37.8和21.5μM（665-COUMATE用作参考的IC50值为1.0μM）。化合物9r对雌激素受体阳性（ER +）细胞系MCF-7表现出最高的效价，GI（50）值为24.7μM。合成的香豆素衍生物与STS酶的结构活性关系为讨论过。

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