Novel pyrazolopyrimidine urea derivatives: Synthesis, antiproliferative activity, VEGFR‐2 inhibition, and effects on the cell cycle profile
Sign Up to like & getrecommendations! Published in 2020 at "Archiv der Pharmazie"
DOI: 10.1002/ardp.201900319
Abstract: A series of novel diaryl urea pyrazolopyrimidine derivatives was designed and synthesized. All the synthesized compounds were evaluated for cytotoxic activity by the National Cancer Institute. A significant antiproliferative activity at a 10‐µM dose was… read more here.
Keywords: cell cycle; pyrazolopyrimidine; antiproliferative activity; vegfr ... See more keywords
Synthesis of novel 2‐acetamide‐5‐phenylthio‐1,3,4‐thiadiazole‐containing phenyl urea derivatives as potential VEGFR‐2 inhibitors
Sign Up to like & getrecommendations! Published in 2022 at "Archiv der Pharmazie"
DOI: 10.1002/ardp.202100397
Abstract: A novel series of 2‐acetamide‐5‐phenylthio‐1,3,4‐thiadiazol derivatives containing a phenyl urea warhead were synthesized and evaluated as antiproliferative agents. The cytotoxic activities of the newly synthesized compounds were evaluated toward three human cancer cell lines, including… read more here.
Keywords: novel acetamide; synthesis novel; acetamide phenylthio; vegfr ... See more keywords
2‐Phenylquinazolin‐4(3H)‐one scaffold as newly designed, synthesized VEGFR‐2 allosteric inhibitors with potent cytotoxicity through apoptosis
Sign Up to like & getrecommendations! Published in 2023 at "Archiv der Pharmazie"
DOI: 10.1002/ardp.202200654
Abstract: New derivatives of 2‐phenylquinazolin‐4(3H)‐one were designed, synthesized, and biologically evaluated as potent allosteric kinase inhibitors with in situ cytotoxicity against MCF‐7 and HepG2 cells. Compounds 15 and 18 among the proposed compounds showed promising antiproliferative… read more here.
Keywords: vegfr; cytotoxicity; apoptosis; phenylquinazolin one ... 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
Design, Synthesis, Docking Studies, and Investigation of Dual EGFR/VEGFR‐2 Inhibitory Potentials of New Pyrazole and Pyrazolopyridine Derivatives
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DOI: 10.1002/ddr.70056
Abstract: The anticancer potential of certain newly synthesized pyrazole and pyrazolopyridine derivatives has been estimated. NCI 60 cancer cells cytotoxic screening pointed out compounds 3e and 3f as the highest cytotoxic agents with % mean growth… read more here.
Keywords: pyrazole pyrazolopyridine; vegfr; egfr vegfr; dual egfr ... See more keywords
Imaging VEGF Receptors and αvβ3 Integrins in a Mouse Hindlimb Ischemia Model of Peripheral Arterial Disease
Sign Up to like & getrecommendations! Published in 2018 at "Molecular Imaging and Biology"
DOI: 10.1007/s11307-018-1191-1
Abstract: PurposeTo compare targeted imaging of vascular endothelial growth factor (VEGF) receptors vs. αvβ3 integrins in a mouse hindlimb ischemia model of peripheral artery disease.ProceduresMale wild-type (WT) C57BL/6 mice (8- to 10-week old) (n = 24) underwent left… read more here.
Keywords: vegf receptors; mouse hindlimb; ischemia model; hindlimb ischemia ... See more keywords
Immunolocalization of VEGF/VEGFR system in human fetal vomeronasal organ during early development.
Sign Up to like & getrecommendations! Published in 2019 at "Acta histochemica"
DOI: 10.1016/j.acthis.2018.11.001
Abstract: The vomeronasal system (VNS) is an accessory olfactory structure present in most mammals adhibited to the detection of specific chemosignals implied in social and reproductive behavior. The VNS comprises the vomeronasal organ (VNO), vomeronasal nerve… read more here.
Keywords: system; vegf; vomeronasal; expression ... See more keywords
Identification of new pyrrolo[2,3-d]pyrimidines as potent VEGFR-2 tyrosine kinase inhibitors: Design, synthesis, biological evaluation and molecular modeling.
Sign Up to like & getrecommendations! Published in 2018 at "Bioorganic chemistry"
DOI: 10.1016/j.bioorg.2018.09.001
Abstract: Vascular endothelial growth factor receptor-2 (VEGFR-2) plays a crucial role in cancer angiogenesis. In the current study, a series of novel pyrrolo[2,3-d]pyrimidine based-compounds was designed and synthesized as VEGFR-2 inhibitors, in accordance to the structure… read more here.
Keywords: kinase inhibitors; pyrrolo pyrimidines; identification new; kinase ... See more keywords
Design, synthesis, and in vitro and in vivo anti-angiogenesis study of a novel vascular endothelial growth factor receptor-2 (VEGFR-2) inhibitor based on 1,2,3-triazole scaffold.
Sign Up to like & getrecommendations! Published in 2020 at "European journal of medicinal chemistry"
DOI: 10.1016/j.ejmech.2020.113083
Abstract: In the past five years, our team had been committed to click chemistry research, exploring the biological activity of 1,2,3-triazole by synthesizing different target inhibitors. In this study, a series of novel indole-2-one derivatives based… read more here.
Keywords: anti angiogenesis; chemistry; compound 13d; vegfr ... See more keywords
Anti-angiogenic effect of a chemically sulfated polysaccharide from Phellinus ribis by inhibiting VEGF/VEGFR pathway.
Sign Up to like & getrecommendations! Published in 2020 at "International journal of biological macromolecules"
DOI: 10.1016/j.ijbiomac.2020.03.068
Abstract: Previous studies have demonstrated that the sulfated polysaccharide named PRP-S16 could inhibit the proliferation, migration, and tube formation of endothelial cells in vitro. Here, its anti-angiogenic effect and mechanism in vivo were investigated by Lewis… read more here.
Keywords: prp s16; vegfr; sulfated polysaccharide; anti angiogenic ... See more keywords
New quinoline-based BODIPYs as EGFR/VEGFR-2 inhibitors: Molecular docking, DFT and in vitro cytotoxicity on HeLa cells
Sign Up to like & getrecommendations! Published in 2022 at "Journal of Molecular Structure"
DOI: 10.1016/j.molstruc.2021.131312
Abstract: Abstract This paper reports quinoline-based BODIPYs as potential EGFR/VEGFR-2 inhibitors and their anticancer activities against Hela cells. Lipinski's drug likeness of compounds 1-3 was predicted revealing that they might exhibit promising physicochemical properties for oral… read more here.
Keywords: egfr vegfr; based bodipys; hela cells; vegfr ... See more keywords