VEGFR-2
VEGFR-2 (vascular endothelial growth factor receptor 2; VEGFR2) is a receptor tyrosine kinase that mediates signaling by vascular endothelial growth factor and has a central role in angiogenesis.
VEGFR-2 (vascular endothelial growth factor receptor 2; VEGFR2) is a receptor tyrosine kinase that mediates signaling by vascular endothelial growth factor and has a central role in angiogenesis. Activation of its kinase domain promotes endothelial-cell responses, including those assessed experimentally by HUVEC tube-formation assays. Because angiogenesis supports tumor development, VEGFR-2 is an important target in anticancer drug discovery, particularly in hepatocellular carcinoma and other cancer models.
Recent studies have focused on synthetic small molecules that inhibit the VEGFR-2 kinase, often in combination with activity against EGFR or PDGFRa. Investigated chemotypes include chalcone–triazole, pyridine–thiazole, quinazoline–chalcone, spiro-oxindoline, indolinone, urea, and hydrazide-hydrazone/thiourea derivatives. Reported evaluations include biochemical kinase inhibition, molecular docking and molecular dynamics simulations, antiproliferative activity, cell-cycle arrest, and effects on apoptosis-related proteins such as BCL2, BAX, TP53, and CASP3. Some compounds were also examined for P-gp inhibition or reversal of cisplatin resistance, while sorafenib served as a comparator in selected studies. These findings place current VEGFR-2 research primarily in the preclinical, discovery-stage development of multi-target anticancer agents.
Where the papers sit
11 papers from the last 6 months study VEGFR-2 directly · updated from PubMed 1 Nov 2026
Study type 0 clinical trials · 1 human data · 10 preclinical
Themes 3 themes
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Dual Kinase Inhibitors and Resistance
Medicinal chemistry is combining VEGFR-2 inhibition with EGFR or P-glycoprotein targeting to strengthen antiproliferative activity and address drug resistance. Pyridine, chalcone, quinazoline and oxindole hybrids are repeatedly evaluated in breast, colorectal and liver cancer cell lines. Cell-cycle arrest and growth inhibition are common endpoints, supported by kinase assays and computational binding studies. Reversal of cisplatin resistance is a specific emerging goal, but the evidence remains largely in vitro.
5 papers · 45.5%
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Apoptosis Induction in Cancer
Multi-targeted small molecules are being developed to inhibit VEGFR-2 alongside PDGFRα or BRAF while directly activating apoptotic death. Urea, benzofuran-thiadiazole and indolinone-based compounds recur across the designs. Antitumor activity is linked to BAX and TP53 signaling, BCL2 suppression and Caspase-3 activation. The evidence remains preclinical, with sorafenib serving as a comparator in several studies and hepatocellular carcinoma as a recurring application.
4 papers · 36.4%
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Structure-Guided Kinase Inhibitor Design
Structure-guided design is being used to optimize anticancer derivatives for binding within the VEGFR-2 kinase domain. Asp1046, Cys919 and Glu885 recur as key interaction sites in docking and molecular-dynamics analyses. Pyrimidine-benzothiazole, phenyl, hydrazide-hydrazone and thiourea scaffolds are paired with synthesis and cell-based testing, especially in MCF-7 and MDA-MB-231 models. The work establishes candidate inhibitors rather than a validated clinical direction, leaving selectivity and in vivo efficacy open.
2 papers · 18.2%
Papers
The 11 papers from the last 6 months that study VEGFR-2 directly, newest first, by theme and by study type. Study types come from PubMed publication types and MeSH headings.
By theme
Dual Kinase Inhibitors and Resistance (5)
- Design, Synthesis, In Vitro Biological Evaluation, and In Silico Studies of Novel Imidazo[4,5-b]Pyridine-Acrylonitrile-Based Derivatives as VEGFR-2 Inhibitors Against Breast Cancer and Hepatocellular Carcinoma. Drug development research · 16 Sept 2026 PMID 42745397
- New oxa/thiadiazole-chalcone hybrids linked via a clickable 1,2,3-triazole bridge with dual EGFR/VEGFR-2 kinase inhibitory activity and antiproliferative effects. Bioorganic chemistry · 9 Sept 2026 PMID 42715623
- Design, synthesis, molecular docking, ADMET and anticancer evaluation of novel pyridine/thiazole hybrids as dual VEGFR-2 and EGFR kinase inhibitors. Bioorganic chemistry · 3 Sept 2026 PMID 42691879
- Discovery of novel Quinazoline-chalcone hybrids as dual VEGFR-2/P-gp inhibitors to reverse cisplatin resistance in cervical Cancer. Bioorganic chemistry · 20 Aug 2026 PMID 42623911
- Ligand-based design and synthesis of novel 3-spiro-2-oxindoline derivatives as potent VEGFR-2 inhibitors with antiproliferative activity and cell cycle arrest. Bioorganic chemistry · 6 Aug 2026 PMID 42561564
Apoptosis Induction in Cancer (4)
- Discovery of new 1-aryl-3-phenylureas as promising PDGFRa and VEGFR-2 inhibitors and apoptosis inducers. Bioorganic chemistry · 16 Sept 2026 PMID 42748748
- Novel benzofuran-1,3,4-thiadiazole aryl urea hybrids as dual VEGFR-2/BRAF inhibitors: anticancer activity, apoptosis induction, and molecular modeling studies. Bioorganic & medicinal chemistry · 6 Aug 2026 PMID 42561779
- New indolin-2-one and isoindoline-1,3-dione derivatives as potential anti-hepatocellular carcinoma agents targeting VEGFR-2: Synthesis, in vitro, in vivo, and in silico evaluation. Bioorganic chemistry · 13 Jul 2026 PMID 42442295
- Antineoplastic multi-targeted spiro[indoline-3,2'-pyrrolidines] incorporating urea function: Rational design, synthesis and bio-properties studies. Bioorganic chemistry · 27 May 2026 PMID 42202589
Structure-Guided Kinase Inhibitor Design (2)
- Rational design of hybrid hydrazide-hydrazone/thiourea derivatives as potential VEGFR-2 targeting anticancer agents: synthesis, biological evaluation, and mechanistic insights into anticancer activity. Bioorganic chemistry · 18 Sept 2026 PMID 42759396
- Design, synthesis, anticancer evaluation, and molecular dynamics-based computational investigation of novel pyrimidine-benzothiazole/phenyl hybrid-based VEGFR-2-targeted derivatives with antioxidant, DNA nicking, DNA interaction, and cytotoxicity studies. Bioorganic chemistry · 25 Aug 2026 PMID 42641238
By study type
Human data, design not indexed (1)
- Design, Synthesis, In Vitro Biological Evaluation, and In Silico Studies of Novel Imidazo[4,5-b]Pyridine-Acrylonitrile-Based Derivatives as VEGFR-2 Inhibitors Against Breast Cancer and Hepatocellular Carcinoma. Drug development research · 16 Sept 2026 PMID 42745397
Preclinical: animal, cell and lab studies (10)
- Rational design of hybrid hydrazide-hydrazone/thiourea derivatives as potential VEGFR-2 targeting anticancer agents: synthesis, biological evaluation, and mechanistic insights into anticancer activity. Bioorganic chemistry · 18 Sept 2026 PMID 42759396
- Discovery of new 1-aryl-3-phenylureas as promising PDGFRa and VEGFR-2 inhibitors and apoptosis inducers. Bioorganic chemistry · 16 Sept 2026 PMID 42748748
- New oxa/thiadiazole-chalcone hybrids linked via a clickable 1,2,3-triazole bridge with dual EGFR/VEGFR-2 kinase inhibitory activity and antiproliferative effects. Bioorganic chemistry · 9 Sept 2026 PMID 42715623
- Design, synthesis, molecular docking, ADMET and anticancer evaluation of novel pyridine/thiazole hybrids as dual VEGFR-2 and EGFR kinase inhibitors. Bioorganic chemistry · 3 Sept 2026 PMID 42691879
- Design, synthesis, anticancer evaluation, and molecular dynamics-based computational investigation of novel pyrimidine-benzothiazole/phenyl hybrid-based VEGFR-2-targeted derivatives with antioxidant, DNA nicking, DNA interaction, and cytotoxicity studies. Bioorganic chemistry · 25 Aug 2026 PMID 42641238
- Discovery of novel Quinazoline-chalcone hybrids as dual VEGFR-2/P-gp inhibitors to reverse cisplatin resistance in cervical Cancer. Bioorganic chemistry · 20 Aug 2026 PMID 42623911
- Novel benzofuran-1,3,4-thiadiazole aryl urea hybrids as dual VEGFR-2/BRAF inhibitors: anticancer activity, apoptosis induction, and molecular modeling studies. Bioorganic & medicinal chemistry · 6 Aug 2026 PMID 42561779
- Ligand-based design and synthesis of novel 3-spiro-2-oxindoline derivatives as potent VEGFR-2 inhibitors with antiproliferative activity and cell cycle arrest. Bioorganic chemistry · 6 Aug 2026 PMID 42561564
- New indolin-2-one and isoindoline-1,3-dione derivatives as potential anti-hepatocellular carcinoma agents targeting VEGFR-2: Synthesis, in vitro, in vivo, and in silico evaluation. Bioorganic chemistry · 13 Jul 2026 PMID 42442295
- Antineoplastic multi-targeted spiro[indoline-3,2'-pyrrolidines] incorporating urea function: Rational design, synthesis and bio-properties studies. Bioorganic chemistry · 27 May 2026 PMID 42202589
Written from 11 PubMed abstracts, each one listed by PMID above. Published: 2026-10-16. Drafted by language models from published abstracts; not medical advice.