| Literature DB >> 17123821 |
Yu Mi Ahn1, Lakshminarayana Vogeti, Chun-Jing Liu, Hari K R Santhapuram, Jonathan M White, Veena Vasandani, Lester A Mitscher, Gerald H Lushington, Paul R Hanson, Douglas R Powell, Richard H Himes, Katherine F Roby, Qizhuang Ye, Gunda I Georg.
Abstract
The design and synthesis of a small library of 8-amidoflavone, 8-sulfonamidoflavone, 8-amido-7-hydroxyflavone, and heterocyclic analogues of flavopiridol is reported. The potential activity of these compounds as kinase inhibitors was evaluated by cytotoxicity studies in MCF-7 and ID-8 cancer cell lines and inhibition of CDK2-Cyclin A enzyme activity in vitro. The antiproliferative and CDK2-Cyclin A inhibitory activity of these analogues was significantly lower than the activity of flavopiridol. Molecular docking simulations were carried out and these studies suggested a different binding orientation inside the CDK2 binding pocket for these analogues compared to flavopiridol.Entities:
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Year: 2006 PMID： 17123821 PMCID： PMC1876666 DOI： 10.1016/j.bmc.2006.10.063
Source DB: PubMed Journal: Bioorg Med Chem ISSN： 0968-0896 Impact factor: 3.641