A comprehensive review of N-heterocycles as cytotoxic agents

D Kumar, S Kumar Jain - Current Medicinal Chemistry, 2016 - ingentaconnect.com
Scientific community is striving to understand the role of heterocycles and fused
heterocycles in drug discovery programme due to its impact on multi-drug resistance (MDR) …

Targeting EGFR and HER‐2 receptor tyrosine kinases for cancer drug discovery and development

S Kamath, JK Buolamwini - Medicinal research reviews, 2006 - Wiley Online Library
Conventional anticancer therapy using cytotoxic drugs lacks selectivity and is prone to
toxicity and drug resistance. Anticancer therapies targeting aberrant growth factor receptor …

GraphEGFR: Multi‐task and transfer learning based on molecular graph attention mechanism and fingerprints improving inhibitor bioactivity prediction for EGFR family …

B Boonyarit, N Yamprasert… - Journal of …, 2024 - Wiley Online Library
The proteins within the human epidermal growth factor receptor (EGFR) family, members of
the tyrosine kinase receptor family, play a pivotal role in the molecular mechanisms driving …

Synthesis and biological activity of novel N-cycloalkyl-(cycloalkylaryl)-2-[(3-R-2-oxo-2H-[1, 2, 4] triazino [2, 3-c] quinazoline-6-yl) thio] acetamides

GG Berest, OY Voskoboynik, SI Kovalenko… - European journal of …, 2011 - Elsevier
In this paper the novel N-cycloalkyl-(cycloalkylaryl)-2-[(3-R-2-oxo-2H-[1, 2, 4] triazino [2, 3-c]
quinazoline-6-yl) thio] acetamides synthesis by aminolysis of activated by thionyl chloride or …

Virtual screening of selective multitarget kinase inhibitors by combinatorial support vector machines

XH Ma, R Wang, CY Tan, YY Jiang, T Lu… - Molecular …, 2010 - ACS Publications
Multitarget agents have been increasingly explored for enhancing efficacy and reducing
countertarget activities and toxicities. Efficient virtual screening (VS) tools for searching …

Synthesis and study of antiproliferative activity of novel thienopyrimidines on glioblastoma cells

S Pédeboscq, D Gravier, F Casadebaig, G Hou… - European journal of …, 2010 - Elsevier
The receptor tyrosine kinases (for example EGFR, PDGFR, VEGFR) are a transmembrane
protein family which plays a crucial role in tumor growth, survival, metastasis dissemination …

QSAR-based models for designing quinazoline/imidazothiazoles/pyrazolopyrimidines based inhibitors against wild and mutant EGFR

JS Chauhan, SK Dhanda, D Singla… - PloS one, 2014 - journals.plos.org
Overexpression of EGFR is responsible for causing a number of cancers, including lung
cancer as it activates various downstream signaling pathways. Thus, it is important to control …

Discovery of Potent EGFR Inhibitors With 6-Arylureido-4-anilinoquinazoline Derivatives

M Li, N Xue, X Liu, Q Wang, H Yan, Y Liu… - Frontiers in …, 2021 - frontiersin.org
According to the classical pharmacophore fusion strategy, a series of 6-arylureido-4-
anilinoquinazoline derivatives (Compounds 7a–t) were designed, synthesized, and …

Lapatinib-binding protein kinases in the African trypanosome: identification of cellular targets for kinase-directed chemical scaffolds

S Katiyar, I Kufareva, R Behera, SM Thomas, Y Ogata… - PloS one, 2013 - journals.plos.org
Human African trypanosomiasis is caused by the eukaryotic microbe Trypanosoma brucei.
To discover new drugs against the disease, one may use drugs in the clinic for other …

Synthesis and biological evaluation of substituted 6-alkynyl-4-anilinoquinazoline derivatives as potent EGFR inhibitors

LT Liu, TT Yuan, HH Liu, SF Chen, YT Wu - Bioorganic & medicinal …, 2007 - Elsevier
A series of C-6 or C-3′ alkynyl-substituted 4-anilinoquinazoline derivatives was prepared
straightforwardly by a Sonogashira reaction of the corresponding bromo-substituted 4 …