作为抗白血病药物的苯乙烯基酮双曼尼希碱
bis-Mannich bases of styryl ketones as antileukemic agents.
作者信息
Dimmock J R, Shyam K, Hamon N W, Patil S A, Smith P J
出版信息
Neoplasma. 1985;32(1):85-91.
PMID:3982563
Abstract
A novel series of bis-Mannich bases have been synthesized and evaluated against P388 lymphocytic leukemia in mice. Two compounds showed a perceptible beneficial response in this screen and all the compounds displayed marked murine toxicity. A representative compound inhibited respiration in mitochondria isolated from rat and mouse liver cells by 90% approximately at a dose of 2.5 mumol and it caused a small elevation in mouse liver glutathione equivalent concentrations at 5 mg/kg.
摘要
已经合成了一系列新型的双曼尼希碱，并在小鼠中针对P388淋巴细胞白血病进行了评估。两种化合物在该筛选中显示出明显的有益反应，并且所有化合物都表现出明显的小鼠毒性。一种代表性化合物在剂量为2.5 μmol时，可使从大鼠和小鼠肝细胞分离出的线粒体呼吸抑制约90%，并且在5 mg/kg剂量时可使小鼠肝脏谷胱甘肽等效浓度略有升高。
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