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• W3156158045 abstract "The connection with acute myelogenous leukemia (AML) of dihydroorotate dehydrogenase (hDHODH), a key enzyme in pyrimidine biosynthesis, has attracted significant interest from pharma as a possible AML therapeutic target. We recently discovered compound 1, a potent hDHODH inhibitor (IC50 = 1.2 nM), able to induce myeloid differentiation in AML cell lines (THP1) in the low nM range (EC50 = 32.8 nM) superior to brequinar’s phase I/II clinical trial (EC50 = 265 nM). Herein, we investigate the 1 drug-like properties observing good metabolic stability and no toxic profile when administered at doses of 10 and 25 mg/kg every 3 days for 5 weeks (Balb/c mice). Moreover, in order to identify a backup compound, we investigate the SAR of this class of compounds. Inside the series, 17 is characterized by higher potency in inducing myeloid differentiation (EC50 = 17.3 nM), strong proapoptotic properties (EC50 = 20.2 nM), and low cytotoxicity toward non-AML cells (EC30(Jurkat) > 100 μM)." @default.
• W3156158045 created "2021-04-26" @default.
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• W3156158045 date "2021-04-12" @default.
• W3156158045 modified "2023-10-16" @default.
• W3156158045 title "Targeting Acute Myelogenous Leukemia Using Potent Human Dihydroorotate Dehydrogenase Inhibitors Based on the 2-Hydroxypyrazolo[1,5-<i>a</i>]pyridine Scaffold: SAR of the Biphenyl Moiety" @default.
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• W3156158045 doi "https://doi.org/10.1021/acs.jmedchem.0c01549" @default.
• W3156158045 hasPubMedCentralId "https://www.ncbi.nlm.nih.gov/pmc/articles/8279415" @default.
• W3156158045 hasPubMedId "https://pubmed.ncbi.nlm.nih.gov/33844533" @default.
• W3156158045 hasPublicationYear "2021" @default.
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