Recent Advances in the Discovery of Multitargeted Tyrosine Kinase Inhibitors as Anticancer Agents

ChemMedChem ◽  
2020 ◽  
Author(s):  
Ting Guo ◽  
Shutao Ma
Keyword(s):  
Tyrosine Kinase ◽  
Tyrosine Kinase Inhibitors ◽  
Anticancer Agents ◽  
Kinase Inhibitors ◽  
Recent Advances

Recent advances in Bcr‐Abl tyrosine kinase inhibitors for overriding T315I mutation

2020 ◽  
Author(s):  
Juan Liu ◽  
Yuan Zhang ◽  
Honglin Huang ◽  
Xiaoyong Lei ◽  
Guotao Tang ◽  
...  
Keyword(s):  
Tyrosine Kinase ◽  
Tyrosine Kinase Inhibitors ◽  
Kinase Inhibitors ◽  
Abl Tyrosine Kinase ◽  
Recent Advances ◽  
T315i Mutation

scholarly journals Recent Advances in Discovery of New Tyrosine Kinase Inhibitors Using Computational Methods

Proceedings ◽  
2019 ◽  
Vol 22 (1) ◽  
pp. 44
Author(s):  
Vesna Rastija
Keyword(s):  
Tyrosine Kinase ◽  
Protein Kinases ◽  
Tyrosine Kinase Inhibitors ◽  
Computational Methods ◽  
Chemical Reactions ◽  
Kinase Inhibitors ◽  
Recent Advances

Tyrosine–protein kinases catalyze chemical reactions that. [...]

scholarly journals Brain Metastasis Treatment: The Place of Tyrosine Kinase Inhibitors and How to Facilitate Their Diffusion across the Blood–Brain Barrier

Pharmaceutics ◽  
2021 ◽  
Vol 13 (9) ◽  
pp. 1446
Author(s):  
Eurydice Angeli ◽  
Guilhem Bousquet
Keyword(s):  
Brain Metastases ◽  
Tyrosine Kinase ◽  
Tyrosine Kinase Inhibitors ◽  
Blood Brain Barrier ◽  
Kinase Inhibitors ◽  
Brain Barrier ◽  
Molecular Alterations ◽  
Blood Brain ◽  
Recent Advances ◽  
Breast Cancer Brain Metastases

The incidence of brain metastases has been increasing constantly for the last 20 years, because of better control of metastases outside the brain, and the failure of most drugs to cross the blood–brain barrier at relevant pharmacological concentrations. Recent advances in the molecular biology of cancer have led to the identification of numerous molecular alterations, some of them targetable with the development of specific targeted therapies, including tyrosine kinase inhibitors. In this narrative review, we set out to describe the state-of-the-art in the use of tyrosine kinase inhibitors for the treatment of melanoma, lung cancer, and breast cancer brain metastases. We also report preclinical and clinical pharmacological data on brain exposure to tyrosine kinase inhibitors after oral administration and describe the most recent advances liable to facilitate their penetration of the blood–brain barrier at relevant concentrations and limit their physiological efflux.

Recent advances in structure-based drug design and virtual screening of VEGFR tyrosine kinase inhibitors

Methods ◽  
2015 ◽  
Vol 71 ◽  
pp. 85-91 ◽  
Author(s):  
Pui Man Hoi ◽  
Shang Li ◽  
Chi Teng Vong ◽  
Hisa Hui Ling Tseng ◽  
Yiu Wa Kwan ◽  
...  
Keyword(s):  
Virtual Screening ◽  
Drug Design ◽  
Tyrosine Kinase ◽  
Tyrosine Kinase Inhibitors ◽  
Kinase Inhibitors ◽  
Structure Based Drug Design ◽  
Recent Advances

scholarly journals In Silico Screening for Novel Tyrosine Kinase Inhibitors With Oxindole Scaffold as Anticancer Agents: Design, QSAR Analysis, Molecular Docking and ADMET Studies

2021 ◽  
Author(s):  
Jalalaldin Zangeneh ◽  
Pouria Shirvani ◽  
Mahmoud Etebari ◽  
lofollah saghaie
Keyword(s):  
Molecular Docking ◽  
Tyrosine Kinase ◽  
Tyrosine Kinase Inhibitors ◽  
Anticancer Agents ◽  
Inhibitory Activity ◽  
Kinase Inhibitors ◽  
Kinase Inhibitor ◽  
Structural Characteristics ◽  
Growth Factor Signaling ◽  
Data Set

Abstract Recently, Anti-cancer targeting drugs are directed against specific molecules and signaling pathways. These targeting agents have reasonable specificity, efficacy, and less side effects. Tyrosine kinases, which play an essential role in growth factor signaling regulation, are significant targets in this type of therapy. Synthesized numerous tyrosine kinase inhibitors (TKIs), such as substituted indolin-2-ones, are effective as anti-tumor and anti-leukemia agents.In this study, a series of novel substituted indolin-2-ones were studied as kinase inhibitor analogs through quantitative structure-activity relationship (QSAR) analysis.Two chemometrics methods, such as multiple linear regression (MLR) and partial least squares combined with genetic algorithm for variable selection (GA-PLS), were employed to establish relationships between structural characteristics and kinase inhibitory activity of oxindole analogs. The GA-PLS was developed as the best predictor and validated QSAR model. The data set compounds were also studied by molecular docking to investigate their binding mechanism in the active site of tyrosine kinase enzymes. According to the information obtained from QSAR models and molecular docking analysis, 44 new potent lead compounds with novel structural features were introduced. Molecular docking, drug-likeness rules, ADMET analysis, bioavailability, toxicity prediction, and target identification were carried out on the newly designed oxindoles to elucidate the fundamental structural properties that affect their inhibitory activity. The results of our study could provide significant insight for future design and development of novel tyrosine kinase inhibitors.

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