Design, synthesis, in silico and antiproliferative evaluation of novel pyrazole derivatives as VEGFR‐2 inhibitors
Sign Up to like & getrecommendations! Published in 2018 at "Archiv der Pharmazie"
DOI: 10.1002/ardp.201700234
Abstract: As the blockade of the VEGFR‐2 signaling pathway is a viable approach in cancer therapy, the present study focuses on a series of pyrazole based VEGFR‐2 inhibitors that were designed on the basis of the… read more here.
Keywords: design synthesis; evaluation novel; synthesis silico; vegfr inhibitors ... See more keywords
Design, synthesis, docking, ADMET profile, and anticancer evaluations of novel thiazolidine‐2,4‐dione derivatives as VEGFR‐2 inhibitors
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DOI: 10.1002/ardp.202000491
Abstract: The anticancer activity of novel thiazolidine‐2,4‐diones was evaluated against HepG2, HCT‐116, and MCF‐7 cells. Among the tested cancer cell lines, HCT‐116 was the most sensitive one to the cytotoxic effect of the new derivatives. In… read more here.
Keywords: hct 116; vegfr inhibitors; admet profile; anticancer ... See more keywords
Design, Development of Pyrazole‐Linked Spirocyclopropyl Oxindole‐Carboxamides as Potential Cytotoxic Agents and Type III Allosteric VEGFR‐2 Inhibitors
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DOI: 10.1002/cmdc.202400422
Abstract: Tumor progression depends on angiogenesis, which is stimulated by growth factors like VEGF, targeting VEGFR kinase with small molecules is an effective anti‐angiogenic therapeutic approach. The rational modification of sunitinib (VEGFR‐2 inhibitor) to spirocyclopropyloxindoline carboxamides… read more here.
Keywords: iii allosteric; type iii; vegfr inhibitors; vegfr ... See more keywords
Discovery of Novel Potent VEGFR-2 Inhibitors Exerting Significant Antiproliferative Activity against Cancer Cell Lines.
Sign Up to like & getrecommendations! Published in 2018 at "Journal of medicinal chemistry"
DOI: 10.1021/acs.jmedchem.7b01091
Abstract: Computational and experimental studies were applied to the discovery of a series of novel vascular endothelial growth factor receptor 2 (VEGFR-2) inhibitors. Eight compounds exhibited nanomolar IC50 values against VEGFR-2, and compounds 6, 19, 22,… read more here.
Keywords: cell lines; vegfr inhibitors; cancer cell; cancer ... See more keywords
An updated patent review of VEGFR-2 inhibitors (2017-present)
Sign Up to like & getrecommendations! Published in 2021 at "Expert Opinion on Therapeutic Patents"
DOI: 10.1080/13543776.2021.1935872
Abstract: ABSTRACT Introduction: Angiogenesis is a vital process for cellular functions in both physiological and pathophysiological conditions and is one of the hallmarks of cancer progression and metastasis. VEGF/VEGFR-2 signaling pathway has been recognized as the… read more here.
Keywords: patent review; review vegfr; updated patent; vegfr inhibitors ... See more keywords
Benzoxazole derivatives as new VEGFR-2 inhibitors and apoptosis inducers: design, synthesis, in silico studies, and antiproliferative evaluation
Sign Up to like & getrecommendations! Published in 2022 at "Journal of Enzyme Inhibition and Medicinal Chemistry"
DOI: 10.1080/14756366.2022.2103552
Abstract: Abstract In this study, a set of novel benzoxazole derivatives were designed, synthesised, and biologically evaluated as potential VEGFR-2 inhibitors. Five compounds (12d, 12f, 12i, 12l, and 13a) displayed high growth inhibitory activities against HepG2… read more here.
Keywords: compound 12l; evaluation; vegfr inhibitors; new vegfr ... See more keywords
New quinoline and isatin derivatives as apoptotic VEGFR-2 inhibitors: design, synthesis, anti-proliferative activity, docking, ADMET, toxicity, and MD simulation studies
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DOI: 10.1080/14756366.2022.2110869
Abstract: Abstract New quinoline and isatin derivatives having the main characteristics of VEGFR-2 inhibitors was synthesised. The antiproliferative effects of these compounds were estimated against A549, Caco-2, HepG2, and MDA-MB-231. Compounds 13 and 14 showed comparable… read more here.
Keywords: new quinoline; quinoline isatin; isatin derivatives; activity ... See more keywords
Evaluation of oxadiazole-N-phenylacetamide conjugates as VEGFR-2 inhibitors and apoptosis inducers: design, synthesis, anti-proliferative assessment, molecular docking, and dynamics studies.
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DOI: 10.1080/17568919.2025.2594968
Abstract: AIM A novel series of oxadiazole-based derivatives was designed and synthesized as vascular endothelial growth factor receptor-2 (VEGFR-2) inhibitors. METHOD The synthesized compounds were evaluated for their cytotoxic and VEGFR-2 inhibition activities. RESULTS Compound 11i… read more here.
Keywords: vegfr inhibitors; oxadiazole phenylacetamide; phenylacetamide conjugates; evaluation oxadiazole ... See more keywords
Discovery of Novel Pyrimidine Based Small Molecule Inhibitors as VEGFR-2 Inhibitors: Design, Synthesis, and Anti-Cancer Studies.
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DOI: 10.2174/0115734099269413231018065351
Abstract: BACKGROUND Receptor tyrosine kinases (RTKs) are potent oncoproteins in cancer that, when mutated or overexpressed, can cause uncontrolled growth of cells, angiogenesis, and metastasis, making them significant targets for cancer treatment. Vascular endothelial growth factor… read more here.
Keywords: vegfr inhibitors; cancer; compound; cell cycle ... See more keywords
Advances in VEGFR Inhibitors: A Comprehensive Review of Novel Anticancer Agents.
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DOI: 10.2174/0118715206356712241202112641
Abstract: Cancer, characterized by aberrant cell growth, presents a formidable health challenge, impacting millions of individuals worldwide each year. Among the myriad mechanisms facilitating tumor progression, Vascular Endothelial Growth Factor receptors (VEGFR) play a pivotal role… read more here.
Keywords: chemistry; cancer; review; vegfr inhibitors ... See more keywords
Selective vascular endothelial growth factor receptor inhibitors provide limited benefits for metastatic colorectal cancer: a meta-analysis.
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DOI: 10.2174/1381612826666200218095932
Abstract: BACKGROUND Metastatic colorectal cancer (mCRC) is one of the most common and deadly cancers worldwide. For most patients diagnosed with mCRC and managed with 5-fluorouracil (5-FU)/leucovorin plus oxaliplatin (FOLFOX), the median survival time is still… read more here.
Keywords: folfox4; vegfr inhibitors; selective vegfr; rate ... See more keywords