ArticleMolecular diversity2026
Novel pyrazole-oxadiazole-chalcone/oxime hybrids as dual EGFR/VEGFR-2 inhibitors with promising anticancer potential: a comprehensive cytotoxicity evaluation, mechanistic insights and SAR analysis.
Article in Molecular diversity, 2026. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 4 papers.
What it found
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The trial behind it
Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.
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Who cites it
4 citing papers in PubMed.
- Exploration of novel hydroxamic acid-based candidates integrating chalcone scaffold cap as multitarget HDAC inhibitors: design, anti-prostatic cancer assessment,Journal of enzyme inhibition and medicinal chemistry · 2026Article
- 1,3,4-Oxadiazole-sulfonamide hybrids: recent advances in biological activities, structure-activity relationships, and therapeutic applications.RSC advances · 2026Review
- Design, synthesis, and preliminary anticancer evaluation of diphenylpropan-1-one derivatives:RSC advances · 2026Article
- Rational Design, Synthesis, Biological Evaluation, and In Silico Study of N-Cinnamamide/Benzamide-(4-(Substituted Phenyl)-6-(4-Cyclohexylphenyl)pyrimidin-2-Yl) Derivatives as EGFR Inhibitors Targeting EGFRChemical biology & drug design · 2026Article
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Authors and funding
4 authors.
Funding
No grant is acknowledged in the PubMed record.
Abstract
A novel series of pyrazole-1,3,4-oxadiazole hybrids incorporating chalcone/oxime scaffolds (10a-10c, 11a-11c, 12a-12i, 13a-13i, and 14a-14i) was synthesized and subjected to an detailed cytotoxicity profile against the NCI-60 human cancer cell line panel. Several derivatives demonstrated broad-spectrum growth inhibition, with compounds 10b, 11a, and 11b emerging as the most active candidates, exhibiting mean GI₅₀ values in the low micromolar range (4.36-16.4 µM). A deeper biological assessment revealed that these hybrids act as dual inhibitors of EGFR and VEGFR-2, with compound 11b showing the highest potency (IC₅₀ = 26.38 nM and 114.17 nM, respectively). Mechanistic studies further confirmed that 11b induced G2/M phase arrest and triggered apoptotic pathways in MCF-7 cells. The oxime-containing analogs exhibited enhanced nitric oxide (NO) release, a property associated with modulation of angiogenesis and increased susceptibility of cancer cells to apoptosis, contributing to their observed anticancer activity. Molecular docking and structure-activity relationship analysis clarified the binding interactions and substitution patterns governing activity, and both cytotoxicity and mechanistic analyses converged on compound 11b as the most promising lead of the series.
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Registered trials
Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the Socratic graph.