Design and Synthesis of a Novel Covalent Dihydropteridinone Derivative as a Highly Potent and Orally Bioavailable PLK1 Inhibitor for the Treatment of Chronic Myeloid Leukemia

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The research aims to design and synthesize a new covalent PLK1 inhibitor for treating chronic myeloid leukemia.
Designed and synthesized a novel dihydropteridinone derivative.
Evaluated the compound's oral bioavailability and potency as a PLK1 inhibitor.
The novel compound demonstrated significant potency as a PLK1 inhibitor.
Achieved favorable oral bioavailability for potential therapeutic use.

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Assesses a novel PLK1 inhibitor's effectiveness against chronic myeloid leukemia, indicating its potential use in treatment.

as a safe, orally bioavailable, and highly potent PLK1 inhibitor for preclinical development.

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Zhou et al. (2026) studied this question.

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