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Targeting Acute Myelogenous Leukemia Using Potent Human Dihydroorotate Dehydrogenase Inhibitors Based on the 2-Hydroxypyrazolo[1,5-a]pyridine Scaffold: SAR of the Aryloxyaryl Moiety

作者:Stefano Sainas, Marta Giorgis, Paola Circosta, Giulio Poli, Marta Alberti, Alice Passoni, Valentina Gaidano, Agnese Chiara Pippione, Nicoletta Vitale, Davide Bonanni, Barbara Rolando, Alessandro Cignetti, Cristina Ramondetti, Alessia Lanno, Davide M. Ferraris, Barbara Canepa, Barbara Buccinnà, Marco Piccinini, Menico Rizzi, Giuseppe Saglio, Salam Al‐Karadaghi, Donatella Boschi, Riccardo Miggiano, Tiziano Tuccinardi, Marco L. Lolli · 发表于:Journal of Medicinal Chemistry · 年份:2022 · DOI:10.1021/acs.jmedchem.2c00496 · 被引用次数:22 · 研究领域:Biochemical and Molecular Research、HIV/AIDS drug development and treatment、Cytomegalovirus and herpesvirus research

has an extremely low cytotoxicity on non-AML cells as well as MEDS433; it has shown a significant antileukemic activity in vivo in a xenograft mouse model of AML.