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新型哒嗪-4-酮衍生物的合成及体外细胞毒性评价。

Synthesis and in-vitro cytotoxic evaluation of novel pyridazin-4-one derivatives.

机构信息

Laboratory of Organic and Analytical Chemistry, Faculty of Sciences and Technology, Béni-Mellal, Morocco.

出版信息

Arch Pharm (Weinheim). 2010 May;343(5):310-3. doi: 10.1002/ardp.200900290.

Abstract

A new series of N-aryl-4-oxo-1,4-dihydro-pyridazine-3-carboxylic acids has been synthesized by condensation of aryldiazonium with 4-hydroxy-6-methyl-2-pyrone. Some of these compounds exhibited in-vitro cytotoxic activity with moderate to excellent growth inhibition against the murine P815 mastocytoma cell line. Compound 5b showed an important cytotoxic activity against cell line P815 (IC(50 )= 0.40 microg/mL).

摘要

通过芳基重氮与 4-羟基-6-甲基-2-吡喃酮缩合,合成了一系列新型的 N-芳基-4-氧代-1,4-二氢-嘧啶-3-羧酸。其中一些化合物表现出体外细胞毒性活性,对小鼠 P815 肥大细胞瘤细胞系具有中等至优异的生长抑制作用。化合物 5b 对 P815 细胞系表现出重要的细胞毒性活性(IC(50)=0.40μg/mL)。

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