There has been huge progress in the discovery of targeted cancer therapies in recent years.
However, even for the most successful and impactful cancer drugs which have been …

Abstract The 1, 2, 3-triazole ring is a major pharmacophore system among nitrogen-
containing heterocycles. These five-membered heterocyclic motifs with three nitrogen …

Gastrointestinal stromal tumor (GIST) is the most common mesenchymal tumor of the
gastrointestinal tract. The majority of GISTs harbor gain of function mutations in either KIT or …

An analysis of 156 published clinical candidates from the Journal of Medicinal Chemistry
between 2018 and 2021 was conducted to identify lead generation strategies most …

Clinically acquired resistance is a major challenge in cancer therapies with small-molecule
kinase inhibitors (SMKIs). Gatekeeper mutations in the ATP-binding pocket of kinases are …

Compared with traditional therapies, targeted therapy has merits in selectivity, efficacy, and
tolerability. Small molecule inhibitors are one of the primary targeted therapies for cancer …

Angiogenesis, the formation of new blood vessels from the existing vasculature, is pivotal in
the migration, growth, and differentiation of endothelial cells in normal physiological …

Receptor tyrosine kinases play an important role in many cellular processes, and their
dysregulation leads to diseases, most importantly cancer. One such receptor tyrosine kinase …

The fundamental importance of water molecules at drug–protein interfaces is now widely
recognised and a significant feature in structure-based drug design. Experimental methods …

Breast cancer is the most common cancer in women, responsible for over half a million
deaths in 2020. Almost 75% of FDA-approved drugs are mainly nitrogen-and sulfur …