Development and strategies of VEGFR-2/KDR inhibitors (Q34436101)

2 August 2017

title

Development and strategies of VEGFR-2/KDR inhibitors (English)

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2 August 2017

Lingyi Huang

1

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2 August 2017

Zhengui Huang

2

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2 August 2017

Zhiqiang Bai

3

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2 August 2017

Rui Xie

4

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2 August 2017

Liping Sun

5

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2 August 2017

Kejiang Lin

6

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2 August 2017

publication date

1 September 2012

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Future Medicinal Chemistry

2 August 2017

published in

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2 August 2017

volume

4

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2 August 2017

issue

14

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2 August 2017

page(s)

1839-1852

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The vascular endothelial growth factor (VEGF) family: angiogenic factors in health and disease

2 August 2017

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Oncogenic kinase signalling

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Surface comparison of active and inactive protein kinases identifies a conserved activation mechanism

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Through the "gatekeeper door": exploiting the active kinase conformation

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The conformational plasticity of protein kinases

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Non-ATP competitive protein kinase inhibitors as anti-tumor therapeutics

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21 January 2018

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Naphthamides as novel and potent vascular endothelial growth factor receptor tyrosine kinase inhibitors: design, synthesis, and evaluation

21 January 2018

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Analysis of kinase inhibitor selectivity using a thermodynamics-based partition index

21 January 2018

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Structure-guided design of aminopyrimidine amides as potent, selective inhibitors of lymphocyte specific kinase: synthesis, structure-activity relationships, and inhibition of in vivo T cell activation

21 January 2018

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Function of the Src-family kinases, Lck and Fyn, in T-cell development and activation

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Recent kinase and kinase inhibitor X-ray structures: mechanisms of inhibition and selectivity insights

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Crystal structure of the tyrosine kinase domain of the human insulin receptor

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Inhibition of p38 MAP kinase by utilizing a novel allosteric binding site

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The design of drug candidate molecules as selective inhibitors of therapeutically relevant protein kinases

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Active and inactive protein kinases: structural basis for regulation

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Features of selective kinase inhibitors

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Selectively nonselective kinase inhibition: striking the right balance

21 January 2018

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Targeting gastrin-releasing peptide receptors on small cell lung cancer cells with a bispecific molecule that activates polyclonal T lymphocytes

21 January 2018

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AZD2171, a pan-VEGF receptor tyrosine kinase inhibitor, normalizes tumor vasculature and alleviates edema in glioblastoma patients.

21 January 2018

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Discovery and preclinical studies of (R)-1-(4-(4-fluoro-2-methyl-1H-indol-5-yloxy)-5- methylpyrrolo[2,1-f][1,2,4]triazin-6-yloxy)propan- 2-ol (BMS-540215), an in vivo active potent VEGFR-2 inhibitor.

21 January 2018

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Targeting angiogenesis: a review of angiogenesis inhibitors in the treatment of lung cancer

21 January 2018

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Novel 4-anilinoquinazolines with C-7 basic side chains: design and structure activity relationship of a series of potent, orally active, VEGF receptor tyrosine kinase inhibitors

21 January 2018

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AEE788: a dual family epidermal growth factor receptor/ErbB2 and vascular endothelial growth factor receptor tyrosine kinase inhibitor with antitumor and antiangiogenic activity

21 January 2018

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In vivo target modulation and biological activity of CHIR-258, a multitargeted growth factor receptor kinase inhibitor, in colon cancer models

21 January 2018

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Synthesis and initial SAR studies of 3,6-disubstituted pyrazolo[1,5-a]pyrimidines: a new class of KDR kinase inhibitors

21 January 2018

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Exploiting chemical libraries, structure, and genomics in the search for kinase inhibitors

21 January 2018

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CLM94, a novel cyclic amide with anti-VEGFR-2 and antiangiogenic properties, is active against primary anaplastic thyroid cancer in vitro and in vivo.

21 January 2018

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Novel pyrazolopyrimidine derivatives as tyrosine kinase inhibitors with antitumoral activity in vitro and in vivo in papillary dedifferentiated thyroid cancer.

21 January 2018

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Kinase inhibition with BAY 43-9006 in renal cell carcinoma

21 January 2018

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Phase I study of antisense oligonucleotide against vascular endothelial growth factor: decrease in plasma vascular endothelial growth factor with potential clinical efficacy

21 January 2018

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Foretinib (GSK1363089), an orally available multikinase inhibitor of c-Met and VEGFR-2, blocks proliferation, induces anoikis, and impairs ovarian cancer metastasis.

21 January 2018

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Cabozantinib (XL184), a novel MET and VEGFR2 inhibitor, simultaneously suppresses metastasis, angiogenesis, and tumor growth

21 January 2018

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21 January 2018

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Advances in the structural biology, design and clinical development of VEGF-R kinase inhibitors for the treatment of angiogenesis

21 January 2018

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Discovery of novel benzimidazoles as potent inhibitors of TIE-2 and VEGFR-2 tyrosine kinase receptors

21 January 2018

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Small molecule inhibitors of KDR (VEGFR-2) kinase: an overview of structure activity relationships

21 January 2018

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3-amino-benzo[d]isoxazoles as novel multitargeted inhibitors of receptor tyrosine kinases

21 January 2018

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7-Aminopyrazolo[1,5-a]pyrimidines as potent multitargeted receptor tyrosine kinase inhibitors.

21 January 2018

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Discovery of N-(4-(3-amino-1H-indazol-4-yl)phenyl)-N'-(2-fluoro-5-methylphenyl)urea (ABT-869), a 3-aminoindazole-based orally active multitargeted receptor tyrosine kinase inhibitor.

21 January 2018

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Discovery of novel 1,2,3,4-tetrahydroisoquinolines and 3,4-dihydroisoquinoline-1(2H)-ones as potent and selective inhibitors of KDR: synthesis, SAR, and pharmacokinetic properties

21 January 2018

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https://api.crossref.org/works/10.4155%2FFMC.12.121

Evaluation of indazole-based compounds as a new class of potent KDR/VEGFR-2 inhibitors

21 January 2018

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https://api.crossref.org/works/10.4155%2FFMC.12.121

Isoindolinone ureas: a novel class of KDR kinase inhibitors.

21 January 2018

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https://api.crossref.org/works/10.4155%2FFMC.12.121

Thienopyrimidine ureas as novel and potent multitargeted receptor tyrosine kinase inhibitors.

21 January 2018

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https://api.crossref.org/works/10.4155%2FFMC.12.121

A small molecule-kinase interaction map for clinical kinase inhibitors

21 January 2018

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https://api.crossref.org/works/10.4155%2FFMC.12.121

Biphenyl amide p38 kinase inhibitors 4: DFG-in and DFG-out binding modes

21 January 2018

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https://api.crossref.org/works/10.4155%2FFMC.12.121

Kinase domain mutations in cancer: implications for small molecule drug design strategies.

21 January 2018

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https://api.crossref.org/works/10.4155%2FFMC.12.121

GW654652, the pan-inhibitor of VEGF receptors, blocks the growth and migration of multiple myeloma cells in the bone marrow microenvironment

21 January 2018

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E7080, a novel inhibitor that targets multiple kinases, has potent antitumor activities against stem cell factor producing human small cell lung cancer H146, based on angiogenesis inhibition

21 January 2018

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Axitinib is an active treatment for all histologic subtypes of advanced thyroid cancer: results from a phase II study

21 January 2018

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A new class of potent vascular endothelial growth factor receptor tyrosine kinase inhibitors: structure-activity relationships for a series of 9-alkoxymethyl-12-(3-hydroxypropyl)indeno[2,1-a]pyrrolo[3,4-c]carbazole-5-ones and the identification of C

21 January 2018

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https://api.crossref.org/works/10.4155%2FFMC.12.121

8-THP-DHI analogs as potent Type I dual TIE-2/VEGF-R2 receptor tyrosine kinase inhibitors

21 January 2018

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1,4-Dihydroindeno[1,2-c]pyrazoles with acetylenic side chains as novel and potent multitargeted receptor tyrosine kinase inhibitors with low affinity for the hERG ion channel

21 January 2018

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Protein kinases as targets for anticancer agents: from inhibitors to useful drugs

21 January 2018

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Structure-activity relationships for a novel series of pyrido[2,3-d]pyrimidine tyrosine kinase inhibitors

21 January 2018

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https://api.crossref.org/works/10.4155%2FFMC.12.121

Structural basis of inhibitor selectivity in MAP kinases

21 January 2018

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https://api.crossref.org/works/10.4155%2FFMC.12.121

Evolution of a highly selective and potent 2-(pyridin-2-yl)-1,3,5-triazine Tie-2 kinase inhibitor

21 January 2018

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Structural factors contributing to the Abl/Lyn dual inhibitory activity of 3-substituted benzamide derivatives

21 January 2018

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AP24534, a pan-BCR-ABL inhibitor for chronic myeloid leukemia, potently inhibits the T315I mutant and overcomes mutation-based resistance

21 January 2018

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AMN107 (nilotinib): a novel and selective inhibitor of BCR-ABL

21 January 2018

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Design and synthesis of 3-substituted benzamide derivatives as Bcr-Abl kinase inhibitors

21 January 2018

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Structural resemblances and comparisons of the relative pharmacological properties of imatinib and nilotinib

21 January 2018

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Synthesis and structure-activity relationships of (aryloxy)quinazoline ureas as novel, potent, and selective vascular endothelial growth factor receptor-2 inhibitors.

21 January 2018

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https://api.crossref.org/works/10.4155%2FFMC.12.121

Identification of novel p38alpha MAP kinase inhibitors using fragment-based lead generation.

21 January 2018

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Application of fragment-based lead generation to the discovery of novel, cyclic amidine beta-secretase inhibitors with nanomolar potency, cellular activity, and high ligand efficiency

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Design, synthesis, and evaluation of orally active benzimidazoles and benzoxazoles as vascular endothelial growth factor-2 receptor tyrosine kinase inhibitors

21 January 2018

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Discovery of N-phenyl nicotinamides as potent inhibitors of Kdr.

21 January 2018

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Design and synthesis of novel DFG-out RAF/vascular endothelial growth factor receptor 2 (VEGFR2) inhibitors. 1. Exploration of [5,6]-fused bicyclic scaffolds

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Synthesis and biological profile of the pan-vascular endothelial growth factor receptor/tyrosine kinase with immunoglobulin and epidermal growth factor-like homology domains 2 (VEGF-R/TIE-2) inhibitor 11-(2-methylpropyl)-12,13-dihydro-2-methyl-8-(py

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Is there a case for selectively promiscuous anticancer drugs?

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21 January 2018

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Measuring and interpreting the selectivity of protein kinase inhibitors

21 January 2018

1 reference

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Vascular endothelial growth factor receptor KDR tyrosine kinase activity is increased by autophosphorylation of two activation loop tyrosine residues

21 January 2018

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Characterization and kinetic mechanism of catalytic domain of human vascular endothelial growth factor receptor-2 tyrosine kinase (VEGFR2 TK), a key enzyme in angiogenesis

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Differential Binding of Inhibitors to Active and Inactive CDK2 Provides Insights for Drug Design

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21 January 2018

Identifiers

DOI

10.4155/FMC.12.121

1 reference

2 August 2017

1 reference