Chemoproteomics‐aided medicinal chemistry for the discovery of EPHA2 inhibitors
S Heinzlmeir, J Lohse, T Treiber, D Kudlinzki… - …, 2017 - Wiley Online Library
The receptor tyrosine kinase EPHA2 has gained attention as a therapeutic drug target for
cancer and infectious diseases. However, EPHA2 research and EPHA2‐based therapies …
cancer and infectious diseases. However, EPHA2 research and EPHA2‐based therapies …
Synthesis and evaluation of novel 2-pyrrolidone-fused (2-oxoindolin-3-ylidene) methylpyrrole derivatives as potential multi-target tyrosine kinase receptor inhibitors
TH Yang, CI Lee, WH Huang, AR Lee - Molecules, 2017 - mdpi.com
Signaling pathways of VEGFs and PDGFs are crucial in tumor angiogenesis, which is
essential in solid tumor progression and metastasis. This study reports our strategy for …
essential in solid tumor progression and metastasis. This study reports our strategy for …
A Two‐Step Synthesis of 2‐Spiropiperidines
SD Griggs, N Thompson, DT Tape… - … A European Journal, 2017 - Wiley Online Library
A general two‐step synthesis of 2‐spiropiperidines has been developed. δ‐Amino‐β‐
ketoesters can be reacted with cyclic ketones to generate 2‐spiropiperidines in good to …
ketoesters can be reacted with cyclic ketones to generate 2‐spiropiperidines in good to …
Protocol for the Direct Conversion of Lactones to Lactams Mediated by 1, 5, 7-Triazabicyclo [4.4. 0] dec-5-ene: Synthesis of Pyridopyrazine-1, 6-diones
DA Rankic, CM Stiff, CW Am Ende… - The Journal of Organic …, 2017 - ACS Publications
We present an operationally simple lactone-to-lactam transformation utilizing diverse amine
nucleophiles. The key steps of amidation, alcohol activation, and cyclization are all mediated …
nucleophiles. The key steps of amidation, alcohol activation, and cyclization are all mediated …
Bicyclic enol cyclocarbamates inhibit penicillin-binding proteins
P Dockerty, JG Edens, MB Tol, DM Angeles… - Organic & …, 2017 - pubs.rsc.org
Natural products form attractive leads for the development of chemical probes and drugs.
The antibacterial lipopeptide Brabantamide A contains an unusual enol cyclocarbamate and …
The antibacterial lipopeptide Brabantamide A contains an unusual enol cyclocarbamate and …
When chemical proteomics meets medicinal chemistry: Guided drug discovery towards EPHA2 inhibitors
S Heinzlmeir - 2017 - mediatum.ub.tum.de
The receptor tyrosine kinase EPHA2 is involved in many diseases and gained interest as
drug target. Chemical proteomics was used to identify clinical EPHA2 inhibitors, to select a …
drug target. Chemical proteomics was used to identify clinical EPHA2 inhibitors, to select a …