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The role of the methoxy group in approved drugs
D Chiodi, Y Ishihara - European Journal of Medicinal Chemistry, 2024 - Elsevier
The methoxy substituent is prevalent in natural products and, consequently, is present in
many natural product-derived drugs. It has also been installed in modern drug molecules …
many natural product-derived drugs. It has also been installed in modern drug molecules …
The influence of reactive oxygen species on cell cycle progression in mammalian cells
Cell cycle regulation is performed by cyclins and cyclin dependent kinases (CDKs).
Recently, it has become clear that reactive oxygen species (ROS) influence the presence …
Recently, it has become clear that reactive oxygen species (ROS) influence the presence …
Drug-resistant EGFR mutations promote lung cancer by stabilizing interfaces in ligand-free kinase-active EGFR oligomers
Abstract The Epidermal Growth Factor Receptor (EGFR) is frequently found to be mutated in
non-small cell lung cancer. Oncogenic EGFR has been successfully targeted by tyrosine …
non-small cell lung cancer. Oncogenic EGFR has been successfully targeted by tyrosine …
Diacylfuroxans are masked nitrile oxides that inhibit GPX4 covalently
JK Eaton, RA Ruberto, A Kramm… - Journal of the …, 2019 - ACS Publications
GPX4 represents a promising yet difficult-to-drug therapeutic target for the treatment of,
among others, drug-resistant cancers. Although most GPX4 inhibitors rely on a …
among others, drug-resistant cancers. Although most GPX4 inhibitors rely on a …
Structure-Based Approach for the Discovery of Pyrrolo[3,2-d]pyrimidine-Based EGFR T790M/L858R Mutant Inhibitors
S Sogabe, Y Kawakita, S Igaki, H Iwata… - ACS medicinal …, 2013 - ACS Publications
The epidermal growth factor receptor (EGFR) family plays a critical role in vital cellular
processes and in various cancers. Known EGFR inhibitors exhibit distinct antitumor …
processes and in various cancers. Known EGFR inhibitors exhibit distinct antitumor …
[HTML][HTML] Structure and dynamics of the EGF receptor as revealed by experiments and simulations and its relevance to non-small cell lung cancer
ML Martin-Fernandez, DT Clarke, SK Roberts… - Cells, 2019 - mdpi.com
The epidermal growth factor receptor (EGFR) is historically the prototypical receptor tyrosine
kinase, being the first cloned and the first where the importance of ligand-induced dimer …
kinase, being the first cloned and the first where the importance of ligand-induced dimer …
Reversible Michael additions: covalent inhibitors and prodrugs
MH Johansson - Mini reviews in medicinal chemistry, 2012 - ingentaconnect.com
Covalent inhibition is an efficient molecular mechanism for inhibiting enzymes or modulating
the function of proteins and is found in the action of many drugs and biologically active …
the function of proteins and is found in the action of many drugs and biologically active …
Drug design targeting active posttranslational modification protein isoforms
Modern drug design aims to discover novel lead compounds with attractable chemical
profiles to enable further exploration of the intersection of chemical space and biological …
profiles to enable further exploration of the intersection of chemical space and biological …
Amino-derivatives of the sesquiterpene lactone class of natural products as prodrugs
JR Woods, H Mo, AA Bieberich, T Alavanja… - MedChemComm, 2013 - pubs.rsc.org
The sesquiterpene lactone class of natural products displays a diverse array of biological
activities due to the presence of the α-methylene-γ-lactone motif. However, clinical …
activities due to the presence of the α-methylene-γ-lactone motif. However, clinical …
Pyrazolo [3, 4-d] pyrimidine-based dual EGFR T790M/HER2 inhibitors: Design, synthesis, structure–activity relationship and biological activity as potential antitumor …
PF Lamie, AM El-Kalaawy, NSA Latif… - European Journal of …, 2021 - Elsevier
A new series of pyrazolo [3, 4-d] pyrimidine/triazine hybrids 6a-r was designed as antitumor
and anticonvulsant agents. All the prepared compounds were evaluated against colon (HCT …
and anticonvulsant agents. All the prepared compounds were evaluated against colon (HCT …