Photoactivatable Caged Prodrugs of VEGFR-2 Kinase Inhibitors

Photoactivatable Caged Prodrugs of VEGFR-2 Kinase Inhibitors

In this study, we report on the design, synthesis, photokinetic properties and in vitro evaluation of photoactivatable caged prodrugs for the receptor tyrosine kinase VEGFR-2. Highly potent VEGFR-2 inhibitors 1 and 3 were caged by introduction of a photoremovable protecting group (PPG) to yield the...

Full description

Bibliographic Details
Main Authors:	Boris Pinchuk, Rebecca Horbert, Alexander Döbber, Lydia Kuhl, Christian Peifer
Format:	Article
Language:	English
Published:	MDPI AG 2016-04-01
Series:	Molecules
Subjects:	photoactivatable prodrugs caging receptor tyrosine kinase kinase inhibitors VEGFR-2 3,4-diarylmaleimides photoremovable protecting group (PPG)
Online Access:	http://www.mdpi.com/1420-3049/21/5/570

Similar Items

Design, Synthesis, and In Vitro Evaluation of the Photoactivatable Prodrug of the PARP Inhibitor Talazoparib
by: Jiaguo Li, et al.
Published: (2020-01-01)

Photoactivatable Platinum-Based Anticancer Drugs: Mode of Photoactivation and Mechanism of Action
by: Ziwen Dai, et al.
Published: (2020-11-01)

Modulation of Receptor Tyrosine Kinase Activity through Alternative Splicing of Ligands and Receptors in the VEGF-A/VEGFR Axis
by: Megan Stevens, et al.
Published: (2019-03-01)

Molecular Targeting of Epidermal Growth Factor Receptor (EGFR) and Vascular Endothelial Growth Factor Receptor (VEGFR)
by: Nichole E. M. Kaufman, et al.
Published: (2021-02-01)

ESIPT-Based Photoactivatable Fluorescent Probe for Ratiometric Spatiotemporal Bioimaging
by: Xiaohong Zhou, et al.
Published: (2016-10-01)

Reactive Oxygen Species (ROS)-Sensitive Prodrugs of the Tyrosine Kinase Inhibitor Crizotinib
by: Bjoern Bielec, et al.
Published: (2020-03-01)

SYNTHESIS OF NEW PHOTOACTIVATABLE NITROXYL (HNO) DONORS BASED ON THE 6,2-HNM PHOTOTRIGGER
by: Brandle, Greggory C.
Published: (2018)

Photoswitchable Azo- and Diazocine-Functionalized Derivatives of the VEGFR-2 Inhibitor Axitinib
by: Linda Heintze, et al.
Published: (2020-11-01)

Long-wavelength photoremovable protecting groups: On the way to in vivo application
by: Aleksey Yu. Vorobev, et al.
Published: (2020-01-01)

Anlotinib: a novel multi-targeting tyrosine kinase inhibitor in clinical development
by: Guoshuang Shen, et al.
Published: (2018-09-01)

Synthesis of 5-(ethylsulfonyl)-2-methoxyaniline: An important pharmacological fragment of VEGFR2 and other inhibitors
by: Miroslav Murár, et al.
Published: (2013-01-01)

Photoactivatable Fluorogenic Labeling via Turn‐On “Click‐Like” Nitroso‐Diene Bioorthogonal Reaction
by: Bai Li, et al.
Published: (2019-07-01)

Theoretical Investigations on Interactions of Arylsulphonyl Indazole Derivatives as Potential Ligands of VEGFR2 Kinase
by: Kornelia Czaja, et al.
Published: (2020-07-01)

The ACTIVE study protocol: apatinib or placebo plus gefitinib as first-line treatment for patients with EGFR-mutant advanced non-small cell lung cancer (CTONG1706)
by: Zhonghan Zhang, et al.
Published: (2019-11-01)

Fruquintinib: a novel antivascular endothelial growth factor receptor tyrosine kinase inhibitor for the treatment of metastatic colorectal cancer
by: Zhang Y, et al.
Published: (2019-08-01)

Photoactivatable Quantum Dots in Super-Resolution Microscopy of Muscle
by: Akel, Amal
Published: (2010)

Red Photoactivatable Genetic Optical-Indicators
by: Wessal Hussein, et al.
Published: (2020-05-01)

Photorelease of phosphates: Mild methods for protecting phosphate derivatives
by: Sanjeewa N. Senadheera, et al.
Published: (2014-08-01)

Structural Basis for Vascular Endothelial Growth Factor Receptor Activation and Implications for Disease Therapy
by: Faheem Shaik, et al.
Published: (2020-12-01)

TRPM7, Magnesium, and Signaling
by: Zhi-Guo Zou, et al.
Published: (2019-04-01)

Case Report: Gastrointestinal PEComa With TFE3 Rearrangement Treated With Anti-VEGFR TKI Apatinib
by: Jiaming Xu, et al.
Published: (2020-11-01)

Engineering Photoactivatability in Genetically Encoded Voltage and pH Indicators
by: Sungmoo Lee, et al.
Published: (2019-10-01)

Expression, regulation and targeting of receptor tyrosine kinases in esophageal squamous cell carcinoma
by: Manoj Kumar Kashyap, et al.
Published: (2018-02-01)

A synthesis and biological screening of predicted inhibitors of Tyrosine Kinases, e.g. KDR, designed in silico
by: Šramel, Peter
Published: (2017)

Design and synthesis of phthalazine-based compounds as potent anticancer agents with potential antiangiogenic activity via VEGFR-2 inhibition
by: Salwa Elmeligie, et al.
Published: (2019-01-01)

Single-Cell Receptor Quantification of an In Vitro Coculture Angiogenesis Model Reveals VEGFR, NRP1, Tie2, and PDGFR Regulation and Endothelial Heterogeneity
by: Si Chen, et al.
Published: (2019-06-01)

Activity of cabozantinib in radioresistant brain metastases from renal cell carcinoma: two case reports
by: Sylvie Négrier, et al.
Published: (2018-11-01)

Design, Synthesis, and In Vitro Biological Activities of a Bio-Oxidizable Prodrug to Deliver Both ChEs and DYRK1A Inhibitors for AD Therapy
by: Anaïs Barré, et al.
Published: (2019-04-01)

Molecular
by: Vinod G. Ugale, et al.
Published: (2017-05-01)

Splice Variants of the RTK Family: Their Role in Tumour Progression and Response to Targeted Therapy
by: Cherine Abou-Fayçal, et al.
Published: (2017-02-01)

Analysis of VEGF-A/VEGFR1/VEGFR2 gene expression in patients with myelodysplastic syndrome
by: N N Kalitin, et al.
Published: (2017-07-01)

Thiol-Substituted Poly(2-oxazoline)s with Photolabile Protecting Groups—Tandem Network Formation by Light
by: Niklas Jung, et al.
Published: (2020-08-01)

Novel Tyrosine Kinase Targets in Urothelial Carcinoma
by: Javier Torres-Jiménez, et al.
Published: (2021-01-01)

3,4-Difluorobenzocurcumin Inhibits Vegfc-Vegfr3-Erk Signalling to Block Developmental Lymphangiogenesis in Zebrafish
by: Kazuhide S. Okuda, et al.
Published: (2021-06-01)

Mechanisms of acquired resistance to tyrosine kinase inhibitors
by: Yi-fan Chen, et al.
Published: (2011-12-01)

Molecular Pharmacology of VEGF-A Isoforms: Binding and Signalling at VEGFR2
by: Chloe J. Peach, et al.
Published: (2018-04-01)

Discovery of a Novel Class of Covalent Dual Inhibitors Targeting the Protein Kinases BMX and BTK
by: Michael Forster, et al.
Published: (2020-12-01)

A New Classification of Prodrugs: Regulatory Perspectives
by: Kuei-Meng Wu
Published: (2009-10-01)

Receptor Tyrosine Kinase Signaling and Targeting in Glioblastoma Multiforme
by: Manali Tilak, et al.
Published: (2021-02-01)

Tyrosine Kinase Receptors in Oncology
by: Jorge Esteban-Villarrubia, et al.
Published: (2020-11-01)