ArticleJournal of enzyme inhibition and medicinal chemistry2019
Novel thienopyrimidine derivatives as dual EGFR and VEGFR-2 inhibitors: design, synthesis, anticancer activity and effect on cell cycle profile.
Article in Journal of enzyme inhibition and medicinal chemistry, 2019. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 17 papers.
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Who cites it
17 citing papers in PubMed, 67 citations in OpenAlex.
- Pyrazolo[3,4-RSC advances · 2026Article
- An efficient methodological approach for synthesis of selenopyridines: generation, reactions, anticancer activity, EGFR inhibitory activity and molecular docking studies.Molecular diversity · 2025Article
- Advances in VEGFR Inhibitors: A Comprehensive Review of Novel Anticancer Agents.Anti-cancer agents in medicinal chemistry · 2025Review
- Advances in Small-molecule Dual Inhibitors Targeting EGFR and HER2 Receptors as Anti-cancer Agents.Current medicinal chemistry · 2025Review
- New pyrano-pyridine conjugates as potential anticancer agents: design, synthesis and computational studies.Future medicinal chemistry · 2024Article
- Recruitment of hexahydroquinoline as anticancer scaffold targeting inhibition of wild and mutants EGFR (EGFRJournal of enzyme inhibition and medicinal chemistry · 2023Article
- New proapoptotic chemotherapeutic agents based on the quinolone-3-carboxamide scaffold acting by VEGFR-2 inhibition.Scientific reports · 2023Article
- Design, synthesis, and docking studies of novel pyrazole-based scaffolds and their evaluation as VEGFR2 inhibitors in the treatment of prostate cancer.RSC advances · 2023Article
- Design, Synthesis, and Biological Evaluation of 2-Mercaptobenzoxazole Derivatives as Potential Multi-Kinase Inhibitors.Pharmaceuticals (Basel, Switzerland) · 2023Article
- Design and Synthesis of New Hydantoin Acetanilide Derivatives as Anti-NSCLC Targeting EGFRPharmaceuticals (Basel, Switzerland) · 2022Article
- In-Silico Screening of Novel Synthesized Thienopyrimidines Targeting Fms Related Receptor Tyrosine Kinase-3 and Their In-Vitro Biological Evaluation.Pharmaceuticals (Basel, Switzerland) · 2022Article
- A Review on Fused Pyrimidine Systems as EGFR Inhibitors and Their Structure-Activity Relationship.Frontiers in chemistry · 2022Review
- Molecular design, synthesis andJournal of enzyme inhibition and medicinal chemistry · 2021Article
- Discovery of Potent EGFR Inhibitors WithFrontiers in pharmacology · 2021Article
- Design, synthesis and biological evaluation of a new thieno[2,3-Journal of enzyme inhibition and medicinal chemistry · 2020Article
- LDL induces cholesterol loading and inhibits endothelial proliferation and angiogenesis in Matrigels: correlation with impaired angiogenesis during wound healing.American journal of physiology. Cell physiology · 2020Article
- Novel Anticancer Fused Pyrazole Derivatives as EGFR and VEGFR-2 Dual TK Inhibitors.Frontiers in chemistry · 2019Article
Corrections and comments
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Authors and funding
4 authors at 1 institution in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
aimDesign and synthesis of thienopyrimidine derivatives as dual EGFR and VEGFR-2 inhibitors. MATERIAL AND
methodsA series of novel 6,7,8,9-tetrahydro-5H-cyclohepta[4,5]thieno[2,3-d]pyrimidine derivatives with different substituents on C-4 position was synthesized and evaluated for their anticancer activity against MCF-7 cell line. EGFR, VEGFR-2 inhibitory assay, the cell cycle analysis and apoptosis induction ability of the most potent compound 5f were evaluated.
resultsMost of the compounds showed moderate to significant anticancer activity. Compound 5f exhibited the most potent anticancer activity being 1.73- and 4.64-folds more potent than erlotinib and doxorubicin, respectively. Compound 5f showed potent EGFR inhibitory activity being 1.18-folds more potent than reference standard erlotinib and it also showed good VEGFR-2 inhibitory activity at the micromolar level with IC
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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 OpenQuestion graph.