BRAF signaling and targeted therapies in melanoma

N Dhomen, R Marais - Hematology/Oncology Clinics, 2009 - hemonc.theclinics.com
The past decade has seen significant advances in our understanding of the cell signaling
pathways that drive melanoma in humans. These studies have demonstrated that the …

Imidazopyridine-based kinase inhibitors as potential anticancer agents: A review

F Peytam, Z Emamgholipour, A Mousavi, M Moradi… - Bioorganic …, 2023 - Elsevier
Considering the fundamental role of protein kinases in the mechanism of protein
phosphorylation in critical cellular processes, their dysregulation, especially in cancers, has …

Paradox-breaking RAF inhibitors that also target SRC are effective in drug-resistant BRAF mutant melanoma

MR Girotti, F Lopes, N Preece, D Niculescu-Duvaz… - Cancer cell, 2015 - cell.com
BRAF and MEK inhibitors are effective in BRAF mutant melanoma, but most patients
eventually relapse with acquired resistance, and others present intrinsic resistance to these …

Ligand-Promoted meta-C–H Amination and Alkynylation

P Wang, GC Li, P Jain, ME Farmer, J He… - Journal of the …, 2016 - ACS Publications
Using a modified norbornene (methyl bicyclo [2.2. 1] hept-2-ene-2-carboxylate) as a
transient mediator, meta-C–H amination and meta-C–H alkynylation of aniline and phenol …

[BOOK][B] Microwave heating as a tool for sustainable chemistry

NE Leadbeater - 2010 - taylorfrancis.com
Shorter reaction times, higher product yields, and enhanced selectivity are some of the
advantages microwave heating has over conventional methods, causing its use to transition …

Non-ATP competitive protein kinase inhibitors

L Garuti, M Roberti, G Bottegoni - Current medicinal chemistry, 2010 - ingentaconnect.com
Protein kinases represent an attractive target in oncology drug discovery. Most of kinase
inhibitors are ATP-competitive and are called type I inhibitors. The ATP-binding pocket is …

C–H hetero-functionalization of arenes through palladacyclopentane-type intermediates

L Cao, Y Hua, HG Cheng, Q Zhou - Organic Chemistry Frontiers, 2021 - pubs.rsc.org
Recent years have witnessed palladium-catalyzed C–H activation emerging as a versatile
strategy for the construction of valuable scaffolds. Palladacyclopentane-type intermediates …

Designing of kinase hinge binders: A medicinal chemistry perspective

V Sharma, M Gupta - Chemical Biology & Drug Design, 2022 - Wiley Online Library
Protein kinases are key regulators of cellular signaling and play a critical role in
oncogenesis. Inhibitors of protein kinases are pursued by both industry and academia as a …

Synthesis and evaluation of novel GSK-3β inhibitors as multifunctional agents against Alzheimer's disease

XL Shi, JD Wu, P Liu, ZP Liu - European Journal of Medicinal Chemistry, 2019 - Elsevier
To target the multi-facets of Alzheimer's disease (AD), a series of novel GSK-3β inhibitors
containing the 2, 3-diaminopyridine moiety were designed and synthesized. The amide …

Molecular dynamics simulation, free energy calculation and structure-based 3D-QSAR studies of B-RAF kinase inhibitors

Y Yang, J Qin, H Liu, X Yao - Journal of chemical information and …, 2011 - ACS Publications
V600EB-RAF kinase is the most frequent onco-genic protein kinase mutation in melanoma
and is a promising target to treat malignant melanoma. In this work, a molecular modeling …