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5-(2-氧代-3-吲哚叉基)噻唑烷-2,4-二酮-1,3-二曼尼希碱衍生物:合成及其抗白血病活性评价

5-(2-Oxo-3-indolinylidene)thiazolidine-2,4-dione-1,3-di-Mannich base derivatives: synthesis and evaluation for antileukemic activity.

作者信息

Eshba N H, Salama H M

出版信息

Pharmazie. 1985 May;40(5):320-2. doi: 10.1002/chin.198537199.

Abstract

A novel series of 5-(2-oxo-3-indolinylidene)thiazolidine-2,4-dione, having the 1- and 3-positions of the isatin and thiazolidine rings respectively, substituted by various Mannich bases, was prepared. Five compounds were evaluated for antileukemic activity against P388 lymphocytic leukemia in the mouse. The di-Mannich base with a dimethylamino component exhibited the highest activity of the tested compounds. Introduction of bromine into the aromatic moiety of isatin ring (position 5) increased the activity of the parent molecule to a smaller extent.

摘要

制备了一系列新型的5-(2-氧代-3-吲哚基亚甲基)噻唑烷-2,4-二酮,其中异吲哚酮和噻唑烷环的1位和3位分别被各种曼尼希碱取代。对五种化合物进行了抗小鼠P388淋巴细胞白血病的抗白血病活性评估。具有二甲基氨基成分的二曼尼希碱在测试化合物中表现出最高活性。在异吲哚酮环的芳香部分(5位)引入溴,使母体分子的活性有较小程度的提高。

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