[HTML][HTML] Discovering Anti-Cancer Drugs via Computational Methods

W Cui, A Aouidate, S Wang, Q Yu, Y Li… - Frontiers in …, 2020 - frontiersin.org
New drug discovery has been acknowledged as a complicated, expensive, time-consuming,
and challenging project. It has been estimated that around 12 years and 2.7 billion USD, on …

[HTML][HTML] From traditional ethnopharmacology to modern natural drug discovery: A methodology discussion and specific examples

S Pirintsos, A Panagiotopoulos, M Bariotakis… - Molecules, 2022 - mdpi.com
Ethnopharmacology, through the description of the beneficial effects of plants, has provided
an early framework for the therapeutic use of natural compounds. Natural products, either in …

Structure based drug design of crizotinib (PF-02341066), a potent and selective dual inhibitor of mesenchymal–epithelial transition factor (c-MET) kinase and …

JJ Cui, M Tran-Dubé, H Shen, M Nambu… - Journal of medicinal …, 2011 - ACS Publications
Because of the critical roles of aberrant signaling in cancer, both c-MET and ALK receptor
tyrosine kinases are attractive oncology targets for therapeutic intervention. The cocrystal …

Molecular conformations, interactions, and properties associated with drug efficiency and clinical performance among VEGFR TK inhibitors

M McTigue, BW Murray, JH Chen… - Proceedings of the …, 2012 - National Acad Sciences
Analyses of compounds in clinical development have shown that ligand efficient-molecules
with privileged physical properties and low dose are less likely to fail in the various stages of …

1,2-Difunctionalized bicyclo[1.1.1]pentanes: Long–sought-after mimetics for ortho/meta-substituted arenes

JX Zhao, YX Chang, C He, BJ Burke… - Proceedings of the …, 2021 - National Acad Sciences
The development of a versatile platform for the synthesis of 1, 2-difunctionalized bicyclo [1.1.
1] pentanes to potentially mimic ortho/meta-substituted arenes is described. The syntheses …

A review of emerging tyrosine kinase inhibitors as durable treatment of neovascular age-related macular degeneration

N Das, S Chaurasia, RP Singh - Expert Opinion on Emerging Drugs, 2023 - Taylor & Francis
Introduction Current treatment for age-related macular degeneration poses a large burden
on patients and the inability of patients to adhere to this immense burden can lead to worse …

A study of axitinib, a VEGF receptor tyrosine kinase inhibitor, in children and adolescents with recurrent or refractory solid tumors: A Children's Oncology Group phase …

JI Geller, E Fox, BK Turpin, SL Goldstein, X Liu… - Cancer, 2018 - Wiley Online Library
Background Axitinib is an oral small molecule that inhibits receptor tyrosine kinases vascular
endothelial growth factor receptors 1 to 3. A phase 1 and pharmacokinetic (PK) trial …

Designed multiple ligands: basic research vs clinical outcomes

L Costantino, D Barlocco - Current medicinal chemistry, 2012 - ingentaconnect.com
The clinical treatment of multifactorial pathologies (eg cancer, Alzheimer's disease,
psychiatric disorders), is still a major challenge. Many researches have been published …

[HTML][HTML] Approved small-molecule ATP-competitive kinases drugs containing indole/azaindole/oxindole scaffolds: R&D and binding patterns profiling

H Zhang, F He, G Gao, S Lu, Q Wei, H Hu, Z Wu… - Molecules, 2023 - mdpi.com
Kinases are among the most important families of biomolecules and play an essential role in
the regulation of cell proliferation, apoptosis, metabolism, and other critical physiological …

[HTML][HTML] Third generation tyrosine kinase inhibitors and their development in advanced renal cell carcinoma

RM Bukowski - Frontiers in oncology, 2012 - frontiersin.org
Angiogenesis in general and the vascular endothelial growth factor (VEGF) signaling axis in
particular is a validated target in renal cell carcinoma (RCC). Clear-cell carcinoma of the …