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- W2032893243 abstract "A novel series of (E)-1-((2-(1-methyl-1H-imidazol-5-yl) quinolin-4-yl) methylene) thiosemicarbazides was discovered as potent inhibitors of IKKβ. In this Letter we document our early efforts at optimization of the quinoline core, the imidazole and the semithiocarbazone moiety. Most potency gains came from substitution around the 6- and 7-positions of the quinoline ring. Replacement of the semithiocarbazone with a semicarbazone decreased potency but led to some measurable exposure." @default.
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- W2032893243 date "2011-01-01" @default.
- W2032893243 modified "2023-09-27" @default.
- W2032893243 title "A novel series of IKKβ inhibitors part I: Initial SAR studies of a HTS hit" @default.
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- W2032893243 doi "https://doi.org/10.1016/j.bmcl.2010.10.126" @default.
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