Synthesis of Novel Derivatives of 4,6-Diarylpyrimidines and Dihydro-Pyrimidin-4-one and In Silico Screening of Their Anticancer Activity

We synthesized some pyrimidinones, dihydropyrimidinones, and 2,4-diarylsubstituted pyrimidines by combining α-aminoamidines with various saturated carbonyl derivatives and similar compounds. Molecular docking results suggest that certain diaryl derivatives of pyrimidine have a strong binding affinity for PIK3γ. Moreover, diphenyl derivatives of pyrimidine exhibited dual inhibitory activity against PI3K and tubulin, showing promise for the development of next-generation microtubule-targeting agents for use in combination therapies.

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Publication Details

Journal
Current Organic Synthesis
Published
2024-12-06
DOI
https://doi.org/10.2174/0115701794356958241024082646
Citations
1
Primary Topic
Synthesis and biological activity
Type
article
Field-Weighted Citation Impact
0.25
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article

Synthesis of Novel Derivatives of 4,6-Diarylpyrimidines and Dihydro-Pyrimidin-4-one and In Silico Screening of Their Anticancer Activity

Alexander V. Kyrychenko, Валентин А. Чебанов, Oleksandr V. Onipko, Oleksandr V. Buravov et al.
1 citations
Current Organic Synthesis
Synthesis and biological activity
0.25
article

Synthesis of Novel Derivatives of 4,6-Diarylpyrimidines and Dihydro-Pyrimidin-4-one and In Silico Screening of Their Anticancer Activity

Alexander V. Kyrychenko, Валентин А. Чебанов, Oleksandr V. Onipko, Oleksandr V. Buravov, Veronika Stoianova, Eugene S. Gladkov
article en
1 citations

Abstract

We synthesized some pyrimidinones, dihydropyrimidinones, and 2,4-diarylsubstituted pyrimidines by combining α-aminoamidines with various saturated carbonyl derivatives and similar compounds. Molecular docking results suggest that certain diaryl derivatives of pyrimidine have a strong binding affinity for PIK3γ. Moreover, diphenyl derivatives of pyrimidine exhibited dual inhibitory activity against PI3K and tubulin, showing promise for the development of next-generation microtubule-targeting agents for use in combination therapies.

Current Organic SynthesisVol. 22(4)
National Academy of Sciences of Ukraine (UA), State Scientific Institution “Institute for Single Crystals” of National Academy of Sciences of Ukraine (UA), Enamine (Ukraine) (UA), V. N. Karazin Kharkiv National University (UA)
Good health and well-being
Openalex Percentile: Top 46%
Synthesis and biological activity
0.25
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