基于类似物的设计、合成与 3-取代-(亚甲肼基)吲哚啉-2-酮类化合物的抗癌生物评估。
Analogue-based design, synthesis and biological evaluation of 3-substituted-(methylenehydrazono)indolin-2-ones as anticancer agents.
机构信息
Industrial Biotechnology Department, Genetic Engineering and Biotechnology Research Institute (GEBRI), Sadat City University, Egypt.
Faculty of Pharmacy, Department of Pharmaceutical Chemistry, Egyptian Russian University, Badr City, Helwan, Egypt.
出版信息
Eur J Med Chem. 2014 May 6;78:275-80. doi: 10.1016/j.ejmech.2014.03.058. Epub 2014 Mar 19.
The docking studies on CDK2 and GSK-3β inspired us to synthesis a series of indoline-2,3-dione hydrazones 10a-l. Treatment of indoline-2,3-dione derivatives 7a-d with hydrazine gave 3-hydrazonoindolin-2-ones 8a-d which were reacted with the appropriate aldehydes 9a-c to yield 3-substituted-(methylenehydrazono)indolin-2-ones 10a-l. Compounds 10a-l showed a significant anticancer activity against human breast cell line MCF-7. Compounds 10c, f, i exhibited the highest activity almost the same of doxorubicin (IC50 = 6.10 μM) with IC50 = 7.75, 6.75, 6.25 μM, respectively.
CDK2 和 GSK-3β 的对接研究启发我们合成了一系列吲哚啉-2,3-二酮腙 10a-l。将吲哚啉-2,3-二酮衍生物 7a-d 与肼反应得到 3-腙基吲哚啉-2-酮 8a-d，然后将其与适当的醛 9a-c 反应得到 3-取代-(亚甲基腙基)吲哚啉-2-酮 10a-l。化合物 10a-l 对人乳腺癌细胞系 MCF-7 表现出显著的抗癌活性。化合物 10c、f、i 的活性最高，几乎与阿霉素（IC50=6.10 μM）相同，IC50 值分别为 7.75、6.75 和 6.25 μM。
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