Fragment-to-lead medicinal chemistry publications in 2020

IJP De Esch, DA Erlanson, W Jahnke… - Journal of medicinal …, 2021 - ACS Publications
Fragment-based drug discovery (FBDD) continues to evolve and make an impact in the
pharmaceutical sciences. We summarize successful fragment-to-lead studies that were …

Fragment-based approaches to identify RNA binders

BM Suresh, A Taghavi, JL Childs-Disney… - Journal of medicinal …, 2023 - ACS Publications
Although fragment-based drug discovery (FBDD) has been successfully implemented and
well-explored for protein targets, its feasibility for RNA targets is emerging. Despite the …

Nucleic acids as templates and catalysts in chemical reactions: target-guided dynamic combinatorial chemistry and in situ click chemistry and DNA/RNA induced …

P Saha, D Panda, J Dash - Chemical Society Reviews, 2023 - pubs.rsc.org
Nucleic acids play crucial roles in transferring cellular information and gene regulations.
DNA and RNA molecules have been associated with multiple human diseases and thus …

Small molecules targeting viral RNA

G Mathez, V Cagno - International Journal of Molecular Sciences, 2023 - mdpi.com
The majority of antivirals available target viral proteins; however, RNA is emerging as a new
and promising antiviral target due to the presence of highly structured RNA in viral genomes …

Synthesis, in vitro antimicrobial evaluation, and molecular docking studies of new isatin-1, 2, 3-triazole hybrids

T El Malah, H Farag, BA Hemdan, REA Mageid… - Journal of Molecular …, 2022 - Elsevier
Antibiotic resistance is rapidly evolving at an alarming rate, posing a severe threat to
humanity. In an effort to develop compounds with antimicrobial activity, we synthesized a …

RNA‐Selective Small‐Molecule Ligands: Recent Advances in Live‐Cell Imaging and Drug Discovery

KH Chan, Y Wang, BX Zheng, W Long, X Feng… - …, 2023 - Wiley Online Library
RNA structures, including those formed from coding and noncoding RNAs, alternative to
protein‐based drug targets, could be a promising target of small molecules for drug …

Azide–Alkyne “Click” Reaction in Water Using Parts-Per-Million Amine-Functionalized Azoaromatic Cu (I) Complex as Catalyst: Effect of the Amine Side Arm

M Khatua, B Goswami, Kamal, S Samanta - Inorganic Chemistry, 2021 - ACS Publications
A series of Cu (II) complexes, 1–4 and 6, were synthesized through a reaction of amine-
functionalized pincer-like ligands, HL 1, 2, L a, b, and a bidentate ligand L 1 with CuCl2 …

HIV-1 Tat amino acid residues that influence Tat-TAR binding affinity: a scoping review

PT Gotora, R van der Sluis, ME Williams - BMC Infectious Diseases, 2023 - Springer
HIV-1 remains a global health concern and to date, nearly 38 million people are living with
HIV. The complexity of HIV-1 pathogenesis and its subsequent prevalence is influenced by …

Bioorthogonal Chemistry in Translational Research: Advances and Opportunities

R Chaudhuri, S Bhattacharya, J Dash - ChemBioChem, 2023 - Wiley Online Library
Bioorthogonal chemistry is a rapidly expanding field of research that involves the use of
small molecules that can react selectively with biomolecules in living cells and organisms …

Design and implementation of synthetic RNA binders for the inhibition of miR-21 biogenesis

C Maucort, DD Vo, S Aouad, C Charrat… - ACS medicinal …, 2021 - ACS Publications
Targeting RNAs using small molecules is an emerging field of medicinal chemistry and
holds promise for the discovery of efficient tools for chemical biology. MicroRNAs are …