641611-63-4Relevant academic research and scientific papers
A carboxylic acid isostere screen of the DHODH inhibitor Brequinar
DeRatt, Lindsey G.,Christine Pietsch,Tanner, Alexandra,Shaffer, Paul,Jacoby, Edgar,Wang, Weixue,Kazmi, Faraz,Zhang, Xiaochun,Attar, Ricardo M.,Edwards, James P.,Kuduk, Scott D.
, (2020)
Dihydroorotate dehydrogenase (DHODH) enzymatic activity impacts many aspects critical to cell proliferation and survival. Recently, DHODH has been identified as a target for acute myeloid differentiation therapy. In preclinical models of AML, the DHODH inhibitor Brequinar (BRQ) demonstrated potent anti-leukemic activity. Herein we describe a carboxylic acid isostere study of Brequinar which revealed a more potent non-carboxylic acid derivative with improved cellular potency and good pharmacokinetic properties.
PHOSPHODIESTERASE INHIBITOR
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Page/Page column 29; 31, (2008/06/13)
[wherein n represents an integer of from 1 to 4, R1 represents substituted or unsubstituted lower alkyl, -C(=Y)R9 or the like, R2 represents a hydrogen atom, substituted or unsubstituted lower alkyl or the like, R3/s
