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• W2039407934 abstract "The FLT3 kinase represents an attractive target to effectively treat AML. Unfortunately, no FLT3 targeted therapeutic is currently approved. In line with our continued interests in treating kinase related disease for anti-FLT3 mutant activity, we utilized pioneering synthetic methodology in combination with computer aided drug discovery and identified low molecular weight, highly ligand efficient, FLT3 kinase inhibitors. Compounds were analyzed for biochemical inhibition, their ability to selectively inhibit cell proliferation, for FLT3 mutant activity, and preliminary aqueous solubility. Validated hits were discovered that can serve as starting platforms for lead candidates. • A virtual library was screened against kinase crystal structures. • An imidazopyridine-core was found active on the FLT3 tyrosine kinase. • Ligand efficient FLT3 hits were generated with strong biochemical and cell activities." @default.
• W2039407934 created "2016-06-24" @default.
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• W2039407934 date "2015-04-01" @default.
• W2039407934 modified "2023-10-12" @default.
• W2039407934 title "Computer aided drug discovery of highly ligand efficient, low molecular weight imidazopyridine analogs as FLT3 inhibitors" @default.
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• W2039407934 doi "https://doi.org/10.1016/j.ejmech.2015.02.052" @default.
• W2039407934 hasPubMedCentralId "https://www.ncbi.nlm.nih.gov/pmc/articles/4666306" @default.
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