Article
Inhibition of FLT3-ITD Kinase in Acute Myeloid Leukemia by New Imidazo[1,2-b]pyridazine Derivatives Identified by Scaffold Hopping.
Journal of medicinal chemistry - 24 Aug 2023
Břehová Petra, Řezníčková Eva, Škach Kryštof, Jorda Radek, Dejmek Milan, Vojáčková Veronika, Šála Michal, Kovalová Markéta, Dračínský Martin, Dolníková Alexandra, Strmeň Timotej, Kinnertová Monika, Chalupský Karel, Dvořáková Alexandra, Gucký Tomáš, Mertlíková Kaiserová Helena, Klener Pavel, Nencka Radim, Kryštof Vladimír
Abstract excerpt
FLT3 kinase is a potential drug target in acute myeloid leukemia (AML). Patients with FLT3 mutations typically have higher relapse rates and worse outcomes than patients without FLT3 mutations. In this study, we investigated the suitability of various heterocycles as central cores of FLT3 inhibitors, including thieno[3,2-d]pyrimidine, pyrazolo[1,5-a]pyrimidine, imidazo[4,5-b]pyridine, pyrido[4,3-d]pyrimidine, and...
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