Nitrogen-containing flavonoids as CDK1/Cyclin B inhibitors: Design, synthesis, and biological evaluation

A novel series of nitrogen-containing flavonoids 5a– l, 6a, b, and 7a, b were designed and synthesized as cyclin-dependent kinases inhibitors. The representative compounds 5a, 5b, 5e, and 5g showed potent CDK1/Cyclin B inhibitory activities. A novel series of nitrogen-containing flavonoids 5a– l, 6a...

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Veröffentlicht in:Bioorganic & medicinal chemistry letters 2007, Vol.17 (1), p.278-281
Hauptverfasser: Liu, Tao, Xu, Zhongmiao, He, Qiaojun, Chen, Yanhong, Yang, Bo, Hu, Yongzhou
Format: Artikel
Sprache:eng
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Zusammenfassung:A novel series of nitrogen-containing flavonoids 5a– l, 6a, b, and 7a, b were designed and synthesized as cyclin-dependent kinases inhibitors. The representative compounds 5a, 5b, 5e, and 5g showed potent CDK1/Cyclin B inhibitory activities. A novel series of nitrogen-containing flavonoids 5a– l, 6a, b, and 7a, b were designed and synthesized as cyclin-dependent kinases (CDKs) inhibitors. The representative compounds 5a, 5b, 5e, and 5g showed potent CDK1/Cyclin B inhibitory activities. All compounds displayed a significant growth inhibitory action in vitro against Bel-7402, PC-3, ECA-109, A-549, HL-60, and MCF-7 cancer cell lines. Flow cytometry analysis showed that 5b induced apoptosis in PC-3 cells.
ISSN:0960-894X
1464-3405
DOI:10.1016/j.bmcl.2006.07.088