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EE-2-Benzylidene-6-(nitrobenzylidene)cyclohexanones: Syntheses cytotoxicity and an examination of some of their electronic steric and hydrophobic properties

机译:EE-2-苄叉基-6-(硝基苄叉基)环己酮:合成细胞毒性及其某些电子空间和疏水性质的检查

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摘要

Three series of structurally isomeric 2-benzylidene-6-(nitrobenzylidene) cyclohexanones >1–>3 were prepared and evaluated against human Molt/C8 and CEM T-lymphocytes as well as murine L1210 cells. The IC50 values of the majority of compounds are less than 10 μM and in some assays, the figures for >1d and >1e are submicromolar. Correlations were discerned between cytotoxic potencies and the atomic charges on one of the olefinic carbon atoms, the torsion angles between an aryl ring, and the adjacent unsaturated group as well as logP values. Three representative compounds were examined for their effect on respiration in rat liver mitochondria.
机译:制备了三个系列的结构异构的2-亚苄基-6-(硝基亚苄基)环己酮> 1 – > 3 ,并针对人的Molt / C8和CEM T淋巴细胞以及鼠类进行了评估L1210细胞。大多数化合物的IC50值均小于10μM,在某些测定中,> 1d 和> 1e 的数值为亚微摩尔。在细胞毒性效力和烯属碳原子之一上的原子电荷,芳基环与相邻的不饱和基团之间的扭转角以及logP值之间可辨别出相关性。检查了三种代表性化合物对大鼠肝线粒体中呼吸作用的影响。

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