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- W2912261390 abstract "Chemical modulation of the flavonol 2-(benzo[d][1,3]dioxol-5-yl)-chromen-4-one (1), a promising anti-Trypanosomatid agent previously identified, was evaluated through a phenotypic screening approach. Herein, we have performed structure–activity relationship studies around hit compound 1. The pivaloyl derivative (13) showed significant anti-T. brucei activity (EC50 = 1.1 μM) together with a selectivity index higher than 92. The early in vitro ADME-tox properties (cytotoxicity, mitochondrial toxicity, cytochrome P450 and hERG inhibition) were determined for compound 1 and its derivatives, and these led to the identification of some liabilities. The 1,3-benzodioxole moiety in the presented compounds confers better in vivo pharmacokinetic properties than those of classical flavonols. Further studies using different delivery systems could lead to an increase of compound blood levels." @default.
- W2912261390 created "2019-02-21" @default.
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- W2912261390 date "2019-01-29" @default.
- W2912261390 modified "2023-10-02" @default.
- W2912261390 title "SAR Studies and Biological Characterization of a Chromen-4-one Derivative as an Anti-<i>Trypanosoma brucei</i> Agent" @default.
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- W2912261390 doi "https://doi.org/10.1021/acsmedchemlett.8b00565" @default.
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