(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

1 reference

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

cites work

1 reference

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

A VEGF-A splice variant defective for heparan sulfate and neuropilin-1 binding shows attenuated signaling through VEGFR-2.

21 January 2018

1 reference

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

The biology of VEGF and its receptors

21 January 2018

1 reference

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

Vascular endothelial growth factor receptor-2: structure, function, intracellular signalling and therapeutic inhibition

21 January 2018

1 reference

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

Oncogenic kinase signalling

21 January 2018

1 reference

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

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

21 January 2018

1 reference

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

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

21 January 2018

1 reference

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

Small-molecule inhibitors binding to protein kinase. Part II: the novel pharmacophore approach of type II and type III inhibition

21 January 2018

1 reference

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

The conformational plasticity of protein kinases

21 January 2018

1 reference

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

Molecular recognition of protein kinase binding pockets for design of potent and selective kinase inhibitors

21 January 2018

1 reference

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

Binding mode of the 4-anilinoquinazoline class of protein kinase inhibitor: X-ray crystallographic studies of 4-anilinoquinazolines bound to cyclin-dependent kinase 2 and p38 kinase

21 January 2018

1 reference

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

A hot spot for protein kinase inhibitor sensitivity

21 January 2018

1 reference

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

Structural bioinformatics-based design of selective, irreversible kinase inhibitors

21 January 2018

1 reference

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

Rational design of inhibitors that bind to inactive kinase conformations

21 January 2018

1 reference

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

Peptide inhibitors of protein kinases-discovery, characterisation and use

21 January 2018

1 reference

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

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

21 January 2018

1 reference

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

The protein kinase complement of the human genome

21 January 2018

1 reference

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

Evaluation of a series of naphthamides as potent, orally active vascular endothelial growth factor receptor-2 tyrosine kinase inhibitors

21 January 2018

1 reference

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

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

21 January 2018

1 reference

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

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

21 January 2018

1 reference

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

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

1 reference

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

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

21 January 2018

1 reference

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

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

21 January 2018

1 reference

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

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

21 January 2018

1 reference

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

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

21 January 2018

1 reference

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

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

21 January 2018

1 reference

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

Active and inactive protein kinases: structural basis for regulation

21 January 2018

1 reference

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

Features of selective kinase inhibitors

21 January 2018

1 reference

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

Selectively nonselective kinase inhibition: striking the right balance

21 January 2018

1 reference

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

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

21 January 2018

1 reference

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

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

21 January 2018

1 reference

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

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

1 reference

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

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

21 January 2018

1 reference

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

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

1 reference

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

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

1 reference

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

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

21 January 2018

1 reference

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

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

21 January 2018

1 reference

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

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

21 January 2018

1 reference

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

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

1 reference

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

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

21 January 2018

1 reference

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

Kinase inhibition with BAY 43-9006 in renal cell carcinoma

21 January 2018

1 reference

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

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

1 reference

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

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

1 reference

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

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

21 January 2018

1 reference

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

Medullary thyroid carcinoma: molecular signaling pathways and emerging therapies

21 January 2018

1 reference

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

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

21 January 2018

1 reference

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

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

21 January 2018

1 reference

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

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

21 January 2018

1 reference

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

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

21 January 2018

1 reference

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

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

21 January 2018

1 reference

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

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

1 reference

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

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

1 reference

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

1 reference

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

Isoindolinone ureas: a novel class of KDR kinase inhibitors.

21 January 2018

1 reference

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

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

21 January 2018

1 reference

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

A small molecule-kinase interaction map for clinical kinase inhibitors

21 January 2018

1 reference

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

1 reference

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

1 reference

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

1 reference

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

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

1 reference

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

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

21 January 2018

1 reference

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

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

1 reference

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

1 reference

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

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

1 reference

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

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

21 January 2018

1 reference

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

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

21 January 2018

1 reference

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

Structural basis of inhibitor selectivity in MAP kinases

21 January 2018

1 reference

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

1 reference

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

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

21 January 2018

1 reference

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

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

21 January 2018

1 reference

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

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

21 January 2018

1 reference

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

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

21 January 2018

1 reference

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

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

21 January 2018

1 reference

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

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

21 January 2018

1 reference

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

1 reference

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

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

21 January 2018

1 reference

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

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

21 January 2018

1 reference

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

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

21 January 2018

1 reference

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

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

21 January 2018

1 reference

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

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

21 January 2018

1 reference

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

Is there a case for selectively promiscuous anticancer drugs?

21 January 2018

1 reference

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

From single- to multi-target drugs in cancer therapy: when aspecificity becomes an advantage.

21 January 2018

1 reference

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

Measuring and interpreting the selectivity of protein kinase inhibitors

21 January 2018

1 reference

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

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

21 January 2018

1 reference

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

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

21 January 2018

1 reference

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

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

21 January 2018

1 reference

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

21 January 2018

Identifiers

DOI

10.4155/FMC.12.121

1 reference

2 August 2017

1 reference