Abstract
Vascular endothelial growth factor receptor (VEGFR) is an important receptor tyrosine kinase (RTK) in the induction of angiogenesis. Abnormal activation of VEGFR leads to several disorders including cancer. Nowadays, inhibition of VEGFR kinase has been one of the most powerful clinical strategies in cancer treatment and great efforts to design and synthesize small molecular VEGFR inhibitors for cancer research have been made in recent years. This review highlights the major progress and development of them, including their structure and pharmacophore features, biological activities and structure-activity relationships (SAR). Special attentions are paid to the compounds available in market or in advanced clinical stages.
Keywords: Vascular endothelial growth factor receptor, anticancer, inhibitor, angiogenesis, small molecular, VEGF, PlGF, Receptor Tyrosine Kinase, multiple myeloma, hematopoiesis, autophosphorylation, Quinazolines, Quinolines, Vandetanib, NSCLC, 1, PD-153035, Cediranib, KRN633, KRN951, Ki 8751, Valatanib, 12, AAL-993, 13, AMG 706, Phthalazines, Anthranilamides, Oxindoles, Sunitinib, GIST, RCC, Semaxanib, FGFR, AEE788, HUVEC, renal cell carcinoma, Sorafenib, Pazopanib, Axitinib, BMS-605541, X-ray crystallography, molecular modeling assay, VEGFR kinase
Mini-Reviews in Medicinal Chemistry
Title: Recent Progress of Small Molecular VEGFR Inhibitors as Anticancer Agents
Volume: 11 Issue: 1
Author(s): D. Xu, T.-L. Wang, L.-P. Sun and Q.-D. You
Affiliation:
Keywords: Vascular endothelial growth factor receptor, anticancer, inhibitor, angiogenesis, small molecular, VEGF, PlGF, Receptor Tyrosine Kinase, multiple myeloma, hematopoiesis, autophosphorylation, Quinazolines, Quinolines, Vandetanib, NSCLC, 1, PD-153035, Cediranib, KRN633, KRN951, Ki 8751, Valatanib, 12, AAL-993, 13, AMG 706, Phthalazines, Anthranilamides, Oxindoles, Sunitinib, GIST, RCC, Semaxanib, FGFR, AEE788, HUVEC, renal cell carcinoma, Sorafenib, Pazopanib, Axitinib, BMS-605541, X-ray crystallography, molecular modeling assay, VEGFR kinase
Abstract: Vascular endothelial growth factor receptor (VEGFR) is an important receptor tyrosine kinase (RTK) in the induction of angiogenesis. Abnormal activation of VEGFR leads to several disorders including cancer. Nowadays, inhibition of VEGFR kinase has been one of the most powerful clinical strategies in cancer treatment and great efforts to design and synthesize small molecular VEGFR inhibitors for cancer research have been made in recent years. This review highlights the major progress and development of them, including their structure and pharmacophore features, biological activities and structure-activity relationships (SAR). Special attentions are paid to the compounds available in market or in advanced clinical stages.
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Cite this article as:
Xu D., Wang T.-L., Sun L.-P. and You Q.-D., Recent Progress of Small Molecular VEGFR Inhibitors as Anticancer Agents, Mini-Reviews in Medicinal Chemistry 2011; 11 (1) . https://dx.doi.org/10.2174/138955711793564015
DOI https://dx.doi.org/10.2174/138955711793564015 |
Print ISSN 1389-5575 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-5607 |
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