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Article

Discovery of novel enasidenib analogues targeting inhibition of mutant isocitrate dehydrogenase 2 as antileukaemic agents.

Journal of enzyme inhibition and medicinal chemistry - 1 Dec 2023

Khalil Ahmed F, El-Moselhy Tarek F, El-Bastawissy Eman A, Abdelhady Rasha, Younis Nancy S, El-Hamamsy Mervat H

Abstract excerpt

Mutant isocitrate dehydrogenase (IDH) 2 "IDH2m" acquires a neo-enzymatic activity reducing α-ketoglutarate to an oncometabolite, D-2-hydroxyglutarate (2-HG). Three s-triazine series were designed and synthesised using enasidenib as a lead compound. In vitro anticancer screening via National Cancer Institute "NCI" revealed that analogues 6a, 6c, 6d, 7g, and 7l were most potent, with mean growth inhibition...

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Identifiers

PMID: 36629449
DOI: 10.1080/14756366.2022.2157411
PMCID: PMC9848300

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