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首页> 外文期刊>European Journal of Medicinal Chemistry: Chimie Therapeutique >Cytotoxic effects, alkylating properties and molecular modelling of coumarin derivatives and their phosphonic analogues.
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Cytotoxic effects, alkylating properties and molecular modelling of coumarin derivatives and their phosphonic analogues.

机译：香豆素衍生物及其膦酸类似物的细胞毒性作用，烷基化性质和分子模型。

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摘要

The cytotoxic effects and alkylating activity of a series of 3-[1-(alkylamino)-ethylidene]-chroman-2,4-dione (4a-4c), 2-methoxy-3-[1-(alkylamino)-ethylidene]-2,3-dihydro-2,4-dioxo-2lambda(5)-b enzo[e][1,2] oxaphosphinane (5a-5c) and [2-oxo-4-phenyl(alkyl)-2H-chromen-3-yl]-phosphonic acids dimethyl ester (6a-6c) on the two leukemia cell lines HL-60 and NALM-6 have been determined. The test compounds are much more toxic to NALM-6 cells than to HL-60 cells. IC(50) data are up to nine times lower for the NALM-6 than for the HL-60 cell lines. As determined in an in vitro Preussmann test phosphonic derivatives 6a-6c possess very high (+++) alkylating activity, phosphoric derivatives 5a-5c are less active (++) while the derivatives 4a-4c can be included in the group of low activity (+) alkylating agents. Using regression analysis QSAR we found a relationship between biological activity and the physicochemical properties of the test compounds. Their cytotoxic effect increases with an increase of the hydrophobic parameters in the region of the substituents at the 2-, 3- and 4-positions of the benzopyrone skeleton of 4-6.
机译：一系列3- [1-（烷基氨基）-亚乙基] -chroman-2,4-二酮（4a-4c），2-甲氧基-3- [1-（烷基氨基）-亚乙基]的细胞毒性作用和烷基化活性-2,3-二氢-2,4-二氧代-2-lambda（5）-b苯并[e] [1,2]氧杂膦烷（5a-5c）和[2-氧代-4-苯基（烷基）-2H-色烯已经确定了两种白血病细胞系HL-60和NALM-6上的-3-基]-膦酸二甲酯（6a-6c）。测试化合物对NALM-6细胞的毒性比对HL-60细胞的毒性大得多。 NALM-6的IC（50）数据最多比HL-60细胞系低9倍。如在体外Preussmann测试中确定，膦酸酯衍生物6a-6c具有非常高的（+++）烷基化活性，磷衍生物5a-5c的活性较低（++），而衍生物4a-4c可以包括在低级磷酸酯类中活性（+）烷基化剂。使用回归分析QSAR，我们发现了生物活性与受试化合物的理化性质之间的关系。它们的细胞毒性作用随在4-6的苯并吡喃酮骨架的2、3和4位上的取代基区域中疏水参数的增加而增加。

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