Synthesis, biological evaluation, and molecular modeling of natural and unnatural flavonoidal alkaloids, inhibitors of kinases

Journal of Medicinal Chemistry
Thanh Binh NguyenFrançoise Guéritte

Abstract

The screening of the ICSN chemical library on various disease-relevant protein kinases led to the identification of natural flavonoidal alkaloids of unknown configuration as potent inhibitors of the CDK1 and CDK5 kinases. We thus developed an efficient and modular synthetic strategy for their preparation and that of analogues in order to determine the absolute configuration of the active natural flavonoidal alkaloids and to provide further insights on the structure-activity relationships in this series. The structural determinants of the interaction between some flavonoidal alkaloids with specific kinases were also evaluated using molecular modeling.

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Citations

Apr 3, 2014·European Journal of Medicinal Chemistry·Rangappa S KeriR Geetha Balakrishna
Jul 16, 2014·European Journal of Medicinal Chemistry·Manjinder SinghOm Silakari
Aug 25, 2015·Interdisciplinary Sciences, Computational Life Sciences·Namachivayam BalakrishnanNaresh Kandakatla
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Jul 7, 2018·Journal of Agricultural and Food Chemistry·Jian ChengGuan-Hu Bao
Jan 18, 2019·Organic Letters·Aaron Coffin, Joseph M Ready

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