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- W3137916557 abstract "Selective cyclooxygenase-1 (COX-1) inhibition has got into the spotlight with the discovery of COX-1 upregulation in various cancers and the cardioprotective role of COX-1 in control of thrombocyte aggregation. Yet, COX-1-selective inhibitors are poorly explored. Thus, three series of quinazoline derivatives were prepared and tested for their potential inhibitory activity toward COX-1 and COX-2. Of the prepared compounds, 11 exhibited interesting COX-1 selectivity, with 8 compounds being totally COX-1-selective. The IC50 value of the best quinazoline inhibitor was 64 nM. The structural features ensuring COX-1 selectivity were elucidated using in silico modeling." @default.
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- W3137916557 date "2021-03-12" @default.
- W3137916557 modified "2023-10-11" @default.
- W3137916557 title "Synthesis, Inhibitory Activity, and <i>In Silico</i> Modeling of Selective COX-1 Inhibitors with a Quinazoline Core" @default.
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- W3137916557 doi "https://doi.org/10.1021/acsmedchemlett.1c00004" @default.
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