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 …

The influence of reactive oxygen species on cell cycle progression in mammalian cells

EH Verbon, JA Post, J Boonstra - Gene, 2012 - Elsevier
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 …

Drug-resistant EGFR mutations promote lung cancer by stabilizing interfaces in ligand-free kinase-active EGFR oligomers

RS Iyer, SR Needham, I Galdadas, BM Davis… - Nature …, 2024 - nature.com
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 …

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 …

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 …

[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 …

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 …

Drug design targeting active posttranslational modification protein isoforms

F Meng, Z Liang, K Zhao, C Luo - Medicinal research reviews, 2021 - Wiley Online Library
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 …

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 …

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 …