Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
1358914 | Bioorganic & Medicinal Chemistry Letters | 2015 | 5 Pages |
Abstract
Indirubin-3′-monoxime (IM) is a potent cyclin-dependent kinase (CDK) inhibitor. Twenty novel IM derivatives were prepared to investigate the structure–activity relationships (SAR) of this compound class. Six compounds showed significant inhibition against both CDK2/cyclin E1 and CDK9/cyclin T1. The most potent compound 7t exhibited IC50 values at submicromolar level. Preliminary SAR trends were suggested and cytotoxicity of these compounds was investigated. Molecular docking studies on compounds 7l and 7t provided conducive clues for further structural optimization.
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Related Topics
Physical Sciences and Engineering
Chemistry
Organic Chemistry
Authors
Lei Yan, Fangfang Lai, Xiaoguang Chen, Zhiyan Xiao,