Development of Potent Inhibitors of Receptor Tyrosine Kinases by Ligand-Based Drug Design and Target-Biased Phenotypic Screening.

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2018
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Abstract
Pyrazolopyrimidines with potent antiproliferative properties were developed by an adaptive strategy that applies ligand-based design and phenotypic screening iteratively and is informed by biochemical assays. To drive development toward specific oncopathways, compounds were tested against cancer cells that overexpress, or not, AXL kinase. Identified phenotypic hits were found to inhibit oncotargets AXL, RET, and FLT3. Subsequent optimization generated antiproliferative lead compounds with unique selectivity profiles, including selective AXL inhibitors and a highly potent inhibitor of FLT3.
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Authors Myers, Samuel H;Temps, Carolin;Houston, Douglas R;Brunton, Valerie G;Unciti-Broceta, Asier;
Journal Journal of medicinal chemistry
Year 2018
DOI
10.1021/acs.jmedchem.7b01605
URL
Keywords
pyrazolopyrimidine 6-hydrazinyluracil anticancer activities dimethylformamide-dimethylacetal pyrimidotriazine

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