Current Topics in Medicinal Chemistry - Volume 21, Issue 28, 2021

Imidazole has an important five-membered aromatic heterocyclic ring, which is available widely in natural products and synthetic molecules. The special structural characteristics of imidazole ring enable it to bind with a variety of enzymes and receptors through hydrogen bonds, coordination, ion-dipole and cation-π interactions, hydrophobic effects, and Van der Waals forces. These interactions promote several biological activit Read More

Thiazolidinedione, an important heterocyclic ring system, is a pharmacophore and a privileged scaffold in medicinal chemistry. Researchers have shown its potential application as a backbone for inhibitors, as it is involved in anticancer development strategies, cancer progression and metastasis. In this paper, the anticancer activities of thiazolidinedione derivatives were reviewed for the first time with respect to differe Read More

1,3,4-thiadiazole is a five-membered aromatic heterocycle containing two nitrogen atoms and one sulfur atom. As a privileged scaffold, it has its unique chemical properties and biological characteristics. In the design of drugs, they are widely and flexibly applied by medicinal chemists, and many candidates with therapeutic prospects have been developed. In this review, we focus on 1,3,4-thiadiazole derivatives and their var Read More

Peptidomimetics are studied for medicinal application because of their ability to mimic hierarchical structures of peptides and proteins. To break the limitation and expand the peptidomimetics family, a new class of peptidomimetics based on peptide nucleic acids (PNAs) backbone - “γ-AApeptides” was developed. Compared with previous peptidomimetics, γ-AApeptides possess prominent advantages such as resistance Read More

With the rapid development of computer science in scopes of theory, software, and hardware, artificial intelligence (mainly in form of machine learning and more complex deep learning) combined with advanced cheminformatics is playing an increasingly important role in drug discovery process. This development has also facilitated privileged scaffold-related research. By definition, a privileged scaffold is a structure that Read More