Small-molecule kinase inhibitors for the treatment of nononcologic diseases

Z Xie, X Yang, Y Duan, J Han… - Journal of medicinal …, 2021 - ACS Publications
Great successes have been achieved in developing small-molecule kinase inhibitors as
anticancer therapeutic agents. However, kinase deregulation plays essential roles not only …

Targeting mitogen-activated protein kinase-activated protein kinase 2 (MAPKAPK2, MK2): medicinal chemistry efforts to lead small molecule inhibitors to clinical trials

M Fiore, S Forli, F Manetti - Journal of medicinal chemistry, 2016 - ACS Publications
The p38/MAPK-activated kinase 2 (MK2) pathway is involved in a series of pathological
conditions (inflammation diseases and metastasis) and in the resistance mechanism to …

Prodrugs as empowering tools in drug discovery and development: recent strategic applications of drug delivery solutions to mitigate challenges associated with lead …

MAM Subbaiah, J Rautio, NA Meanwell - Chemical Society Reviews, 2024 - pubs.rsc.org
The delivery of a drug to a specific organ or tissue at an efficacious concentration is the
pharmacokinetic (PK) hallmark of promoting effective pharmacological action at a target site …

Discovery of a Potent (4R,5S)-4-Fluoro-5-methylproline Sulfonamide Transient Receptor Potential Ankyrin 1 Antagonist and Its Methylene Phosphate Prodrug …

H Chen, M Volgraf, S Do, A Kolesnikov… - Journal of Medicinal …, 2018 - ACS Publications
Transient receptor potential ankyrin 1 (TRPA1) is a non-selective cation channel expressed
in sensory neurons where it functions as an irritant sensor for a plethora of electrophilic …

Current insights of inhibitors of p38 mitogen-activated protein kinase in inflammation

A Awasthi, MB Raju, MA Rahman - Medicinal Chemistry, 2021 - ingentaconnect.com
Background: The inflammatory process is one of the mechanisms by which our body
upholds us from pathogens such as parasites, bacteria, viruses, and other harmful …

Expanding the repertoire for “large small molecules”: prodrug ABBV-167 efficiently converts to venetoclax with reduced food effect in healthy volunteers

AH Salem, ZF Tao, OF Bueno, J Chen, S Chen… - Molecular Cancer …, 2021 - AACR
Since gaining approval for the treatment of chronic lymphocytic leukemia (CLL), the BCL-2
inhibitor venetoclax has transformed the treatment of this and other blood-related cancers …

[图书][B] Drug Discovery with Privileged Building Blocks: Tactics in Medicinal Chemistry

JJ Li, M Yang - 2021 - taylorfrancis.com
Drug Discovery with Privileged Building Blocks traces back PharmaBlock's founding
philosophy of designing privileged building blocks. High-quality building blocks are crucial …

Pentacoordinated and hexacoordinated compounds

R Pajkert, GV Röschenthaler - 2017 - books.rsc.org
This chapter covers recent developments in the title area published during 2015.
Surprisingly, the past year has seen a significant decrease in the number of papers …

The Total Synthesis of Pseudonocardia sp. Quinolone Natural Products and Studies Towards the Total Synthesis of 1β-Hydroxyalantolactone

SM Geddis - 2019 - repository.cam.ac.uk
Natural products have long been known for their broad range of useful therapeutic
properties, and have been widely utilised in the field of medicine. This dissertation describes …