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• W2317462866 abstract "Substituting a carbon atom with a nitrogen atom (nitrogen substitution) on an aromatic ring in our leads 11a and 13g by applying nitrogen scanning afforded a set of compounds that improved not only the solubility but also the metabolic stability. The impact after nitrogen substitution on interactions between a derivative and its on- and off-target proteins (Raf/MEK, CYPs, and hERG channel) was also detected, most of them contributing to weaker interactions. After identifying the positions that kept inhibitory activity on HCT116 cell growth and Raf/MEK, compound 1 (CH5126766/RO5126766) was selected as a clinical compound. A phase I clinical trial is ongoing for solid cancers." @default.
• W2317462866 created "2016-06-24" @default.
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• W2317462866 date "2014-01-24" @default.
• W2317462866 modified "2023-10-18" @default.
• W2317462866 title "Optimizing the Physicochemical Properties of Raf/MEK Inhibitors by Nitrogen Scanning" @default.
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• W2317462866 doi "https://doi.org/10.1021/ml400379x" @default.
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