Synthesis and in vitro anticancer activity of some 2-oxindoline derivatives as potential CDK2 inhibitors

Name: Synthesis and in vitro anticancer activity of some 2-oxindoline derivatives as potential CDK2 inhibitors
Creator: Taylor & Francis
Published: 2023-03-16T15:20:08+08:00

DataCite Commons2023-12-18 更新2024-08-18 收录

抗癌药物

CDK2抑制剂

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https://tandf.figshare.com/articles/dataset/Synthesis_and_i_in_vitro_i_anticancer_activity_of_some_2-oxindoline_derivatives_as_potential_CDK2_inhibitors/22285503/1 数据链接链接失效反馈

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资源简介：

Novel series of 2-oxindoline hydrazones 6a–h, 3-hydroxy-2-oxoindolines 9a–d and 2-oxoindolin-3-ylidenes 10a–d were prepared and assessed for their anticancer activity towards breast cancer cell line (MCF7). Compounds 6c, 6d, 6g, 9d, 10a and 10b (IC50 = 14.0 ± 0.7, 15.6 ± 0.7, 13.8 ± 0.7, 4.9 ± 0.2, 6.0 ± 0.3 and 10.8 ± 0.5 µM, respectively) showed the highest growth inhibition activity against MCF7 when compared to staurosporine (IC50 = 14.5 ± 0.7 µM). Cell cycle analysis exposed arrest at G1 phase for compounds 6c, 10 and 10b, at S phase for compounds 6d and 9d, and at G1/S phase for compound 6g. Apoptotic effect of compounds 6c, 6d, 6g, 9d, 10a and 10b was confirmed via their early and late apoptotic effects. A safety profile was revealed for compounds 6c, 6d, 6g, 9d, 10a and 10b on MCF10A treated normal cell. Also, compounds 6c and 10b displayed a promising CDK2 inhibition activity (IC50 = 0.22 ± 0.01, 0.25 ± 0.01 µM, respectively). Also, docking study revealed comparable interactions with the native ligand (5-bromoindirubin). ADMET computational studies forecast the promising pharmacokinetic profile of the targeted compounds. Communicated by Ramaswamy H. Sarma

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Taylor & Francis

创建时间：

2023-03-16

Synthesis and <i>in vitro</i> anticancer activity of some 2-oxindoline derivatives as potential CDK2 inhibitors

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