Drugging undruggable molecular cancer targets

JS Lazo, ER Sharlow - Annual review of pharmacology and …, 2016 - annualreviews.org
Cancer, more than any other human disease, now has a surfeit of potential molecular targets
poised for therapeutic exploitation. Currently, a number of attractive and validated cancer …

Unpacking the Pathogen Box—an open source tool for fighting neglected tropical disease

CGL Veale - ChemMedChem, 2019 - Wiley Online Library
Abstract The Pathogen Box is a 400‐strong collection of drug‐like compounds, selected for
their potential against several of the world's most important neglected tropical diseases …

Vinylene carbonate: Beyond the ethyne surrogate in rhodium-catalyzed annulation with amidines toward 4-methylquinazolines

C Wang, X Fan, F Chen, PC Qian… - Chemical …, 2021 - pubs.rsc.org
In this paper, we developed a rhodium-catalyzed annulation of vinylene carbonate with
amidines, leading to 4-methylquinazolines with moderate to excellent yields. This procedure …

Quinazoline ligands induce cancer cell death through selective STAT3 inhibition and G-quadruplex stabilization

J Jamroskovic, M Doimo, K Chand, I Obi… - Journal of the …, 2020 - ACS Publications
The signal transducer and activator of transcription 3 (STAT3) protein is a master regulator of
most key hallmarks and enablers of cancer, including cell proliferation and the response to …

[HTML][HTML] Stimulation of natural killer cells with small molecule inhibitors of CD38 for the treatment of neuroblastoma

CM Mills, TZ Benton, I Piña, MJ Francis, L Reyes… - Chemical …, 2023 - pubs.rsc.org
High-risk neuroblastoma (NB) accounts for 15% of all pediatric cancer deaths. Refractory
disease for high-risk NB patients is attributed to chemotherapy resistance and …

Identification of Compounds that Selectively Stabilize Specific G‐Quadruplex Structures by Using a Thioflavin T‐Displacement Assay as a Tool

J Jamroskovic, M Livendahl, J Eriksson… - … A European Journal, 2016 - Wiley Online Library
Small molecules are used in the G‐quadruplex (G4) research field in vivo and in vitro, and
there are increasing demands for ligands that selectively stabilize different G4 structures …

Nucleophilic aromatic substitution of heterocycles using a high-temperature and high-pressure flow reactor

M Charaschanya, AR Bogdan, Y Wang, SW Djuric - Tetrahedron Letters, 2016 - Elsevier
We report herein a high-temperature and high-pressure continuous-flow protocol to carry out
nucleophilic aromatic substitution (SN Ar) of heterocycles with nitrogen nucleophiles …

Optimization of pyrazole-containing 1, 2, 4-triazolo-[3, 4-b] thiadiazines, a new class of STAT3 pathway inhibitors

MG LaPorte, Z Wang, R Colombo, A Garzan… - Bioorganic & medicinal …, 2016 - Elsevier
Abstract Structure–activity relationship studies of a 1, 2, 4-triazolo-[3, 4-b] thiadiazine
scaffold, identified in an HTS campaign for selective STAT3 pathway inhibitors, determined …

HCS campaign to identify selective inhibitors of IL-6-induced STAT3 pathway activation in head and neck cancer cell lines

PA Johnston, M Sen, Y Hua, DP Camarco… - Assay and drug …, 2015 - liebertpub.com
Signal transducer and activator of transcription factor 3 (STAT3) is hyperactivated in head
and neck squamous cell carcinomas (HNSCC). Cumulative evidence indicates that IL-6 …

I 2-Catalyzed oxidative synthesis of N, 4-disubstituted quinazolines and quinazoline oxides

N Jatangi, RK Palakodety - Organic & Biomolecular Chemistry, 2019 - pubs.rsc.org
An easy and efficient approach to the synthesis of N, 4-disubstituted quinazoline-2-amine
and oxides is described. This transformation proceeds smoothly in the presence of …