Andreani A, Granaiola M, Leoni A, Locatelli A, Morigi R, Rambaldi M, Giorgi G, Salvini L, Garaliene V
Dipartimento di Scienze Farmaceutiche, Università di Bologna, Italy.
Anticancer Drug Des. 2001 Apr-Jun;16(2-3):167-74.
The synthesis of 3-(5-imidazo]2,1-blthiazolylmethylene)-2-indolinones, analogs of compounds recently published, is described. The EIZ isomerism was studied by means of nuclear Overhauser effect experiments and X-ray crystallography. All the compounds were tested as potential antitumor agents. They were also tested as potential inhibitors of cyclin-dependent kinase 1 (CDK1), in order to determine if the antitumor activity was related to this mechanism of action. The results showed that under certain substitution conditions (5-methoxy group for the indole benzene ring and 2-methyl group for the imidazothiazole system), an interesting antitumor activity was found for some compounds. From the analysis of the antitumor data, 3-1(2,6-dimethylimidazo[2,1-bJ-thiazol-5-yl)methylenel-5-methoxy-2-indolinone was the most active of the whole series.
本文描述了3-(5-咪唑并[2,1-b]噻唑基亚甲基)-2-吲哚酮的合成，该化合物是最近发表的化合物类似物。通过核Overhauser效应实验和X射线晶体学研究了E/Z异构现象。所有化合物均作为潜在的抗肿瘤药物进行了测试。它们还作为细胞周期蛋白依赖性激酶1（CDK1）的潜在抑制剂进行了测试，以确定抗肿瘤活性是否与这种作用机制有关。结果表明，在某些取代条件下（吲哚苯环上为5-甲氧基，咪唑并噻唑体系上为2-甲基），一些化合物具有有趣的抗肿瘤活性。通过对抗肿瘤数据的分析，3-[(2,6-二甲基咪唑并[2,1-b]噻唑-5-基)亚甲基]-5-甲氧基-2-吲哚酮是整个系列中活性最高的。
