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This is a In Vitro Study study.

November 28, 2025ChemistryOpenOpen Access

Synthesis of Pyrido2,3‐dAzolopyrimidinones: Design and Epidermal Growth Factor Receptor‐Targeted Molecular Docking Toward Novel Anticancer Leads

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Synthesis of novel anticancer leads shows cytotoxicity comparable to doxorubicin, suggesting effective EGFR targeting.

Cytotoxicity against HepG2 cells showed submicromolar activity, with IC50 values of 0.72–0.95 µM compared to doxorubicin's 0.65 µM.
Molecular docking to the EGFR kinase domain indicated strong binding affinity, with scores from -9.6 to -10.2 kcal mol-1 for top compounds.
Structure–activity trends revealed that certain functionalities enhance the potency of synthesized compounds against cancer cells.
In silico ADMET predictions suggest these pyridopyrimidine scaffolds may offer favorable drug-likeness and non-mutagenic profiles.

Gomha et al. (2025) studied this question.

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November 28, 2025ChemistryOpenOpen Access

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Authors

Synthesis of novel anticancer leads shows cytotoxicity comparable to doxorubicin, suggesting effective EGFR targeting.

Cytotoxicity against HepG2 cells showed submicromolar activity, with IC50 values of 0.72–0.95 µM compared to doxorubicin's 0.65 µM.
Molecular docking to the EGFR kinase domain indicated strong binding affinity, with scores from -9.6 to -10.2 kcal mol-1 for top compounds.
Structure–activity trends revealed that certain functionalities enhance the potency of synthesized compounds against cancer cells.
In silico ADMET predictions suggest these pyridopyrimidine scaffolds may offer favorable drug-likeness and non-mutagenic profiles.

Gomha et al. (2025) studied this question.

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