ArticleBMC chemistry2023
Synthesis of phthalazine-based derivatives as selective anti-breast cancer agents through EGFR-mediated apoptosis: in vitro and in silico studies.
Article in BMC chemistry, 2023. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 8 papers.
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Who cites it
8 citing papers in PubMed.
- Phthalazine as a medically versatile polyheterocyclic core with underexplored anticancer potential.Journal of enzyme inhibition and medicinal chemistry · 2026Review
- Phthalazine scaffolds in medicinal chemistry: a review of their synthesis, versatility, and pharmacological significance.Molecular diversity · 2026Review
- A minimal-net CNN model for an IoT-based brain tumor detection and monitoring system.Scientific reports · 2026Article
- BrainFusionNet: a deep learning and XAI model to understand local, global, and sequential features of MRI images for improved brain tumour detection.Brain informatics · 2026Article
- Recent advances on anticancer activity of benzodiazine heterocycles through kinase inhibition.RSC advances · 2025Review
- CADD Methods for Developing Novel Compounds Synthesized to Inhibit Tyrosine Kinase Receptors.Current topics in medicinal chemistry · 2025Review
- Synthesis of novel phthalazine-based derivatives with potent cytotoxicity against HCT-116 cells through apoptosis and VEGFR2 inhibition.RSC advances · 2024Article
- Synthesis, andCurrent computer-aided drug design · 2024Article
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5 authors.
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Abstract
The parent 2-(4-benzyl-1-oxophthalazin-2(1H)-yl)-acetohydrazide (4) has twenty-nine compounds. The starting material for their corresponding mono, dipeptides and reactions with active methylene compounds were produced by chemoselective N-alkylation of 4-Benzyl-2H-phthalazin-1-one (2) with ethyl chloroacetate to afford (4-benzyl-1-oxo-1H-phthalazin-2-yl) methyl acetate (3). The ester 3 was hydrazinolyzed to give hydrazide 4, then azide 5 coupled with amino acid ester hydrochloride and/or amines to produce several monopeptides, then the methyl (2-(4-benzyl-1-oxophthalazin-2(1H)-yl) acetyl) glycinate (7a) was hydrazinolyzed to produce corresponding hydrazide 2-(4-benzyl-1-oxophthalazin-2(1H)-yl)-N-(2-hydrazineyl-2-oxo ethyl) acetamide (8a). The hydrazide 8a under azide coupling method was coupled with amino acid ester hydrochloride and/or amines to produce several dipeptides, and the hydrazide 8a was also condensed and/or cyclized with several carbonyl compounds. The cytotoxicity of the synthesized compounds was tested using MTT assay, as well as apoptosis-induction through EGFR inhibition. Compounds 11d, 12c and 12d exhibited potent cytotoxic activities with IC
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