吡咯并[3,4-d]哒嗪酮的新型衍生物及其抗癌作用。
New derivatives of pyrrolo[3,4-d]pyridazinone and their anticancer effects.
作者信息
Malinka Wiesław, Redzicka Aleksandra, Lozach Olivier
机构信息
Department of Chemistry of Drugs, Wrocław Medical University, ul.Tamka 1, Wrocław 50-137, Poland.
出版信息
Farmaco. 2004 Jun;59(6):457-62. doi: 10.1016/j.farmac.2004.03.002.
Eighteen new derivatives of pyrrolo[3,4-d]pyridazinone modified at the pyrrole and pyridazine rings were synthesized and 12 of them were evaluated in vitro through anticancer screenings. The structures of new compounds were confirmed by elemental analysis and spectral data (IR, 1H NMR). None of the eight compounds assayed blocked the cell cycle regulating CDK1/cyclin B kinase, whereas two of the six compounds tested were active in anticancer screening at the cell experiments at a concentration of > or = 10(-5) M/l.
合成了18种在吡咯环和哒嗪环上修饰的吡咯并[3,4-d]哒嗪酮新衍生物，并对其中12种进行了体外抗癌筛选。通过元素分析和光谱数据（红外光谱、核磁共振氢谱）确定了新化合物的结构。所检测的8种化合物均未阻断细胞周期调节CDK1/细胞周期蛋白B激酶，而所测试的6种化合物中有2种在细胞实验中浓度≥10(-5)M/L时具有抗癌活性。
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