Novel Mechanism of Decyanation of GDC-0425 by Cytochrome P450
نویسندگان
چکیده
منابع مشابه
Novel Mechanism of Decyanation of GDC-0425 by Cytochrome P450.
GDC-0425 [5-((1-ethylpiperidin-4-yl)oxy)-9H-pyrrolo[2,3-b:5,4-c']dipyridine-6-carbonitrile] is an orally bioavailable small-molecule inhibitor of checkpoint kinase 1 that was investigated as a novel cotherapy to potentiate chemotherapeutic drugs, such as gemcitabine. In a radiolabeled absorption, distribution, metabolism, and excretion study in Sprague-Dawley rats, trace-level but long-lived 14...
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متن کاملMechanism of oxidation reactions catalyzed by cytochrome p450 enzymes.
ion phase that leads to an alkyl radical coordinated to the iron-hydroxo complex by a weak OH---C hydrogen bond, labeled as CI; (ii) an alkyl (or OH) rotation phase whereby the alkyl group achieves a favorable orientation for rebound; and (iii) a rebound phase that leads to C-O bond making and the ferric-alcohol complexes, 4,2P. The two profiles remain close in energy throughout the first two p...
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ژورنال
عنوان ژورنال: Drug Metabolism and Disposition
سال: 2017
ISSN: 0090-9556,1521-009X
DOI: 10.1124/dmd.116.074336