Identification of 2-arylquinazolines with alkyl-polyamine motifs as potent antileishmanial agents: Synthesis and biological evaluation studies

2-Arylquinazolines with a range of alkyl polyamines as side chain/ring functional motifs at 4th-position were considered for antileishmanial study with the rationale that related heterocyclic scaffolds and the polyamine functionalities...

Target 2035 – update on the quest for a probe for every protein

Twenty years after the publication of the first draft of the human genome, our knowledge of the human proteome is still fragmented. Target 2035 aims to develop a pharmacological modulator for every protein in the human proteome to fill this gap.

Bifunctional Chelators for Radiorhenium: Past, Present and Future Outlook

Targeted radionuclide therapy (TRNT) is an ever-expanding field of nuclear medicine that provides a personalised approach to cancer treatment while limiting toxicity to normal tissues. It involves the radiolabelling of...

Identification of the first structurally validated covalent ligands of the small GTPase RAB27A

A novel Rab27A construct enables elucidation of covalent ligand binding, paving the way for structure-guided approaches against this challenging target.

Design, Synthesis and Anti-mycobacterial Evaluation of Imidazo-[1,2-a]-pyridine Analogues

Based on the molecular hybridization strategy, thirty-four imidazo-[1,2-a]-pyridine amide (IPA) and imidazo-[1,2-a]-pyridine sulfonamide (IPS) were designed and synthesized. The structures of the target compounds were characterized using 1 HNMR, 13...

Development of 2-deoxystreptamine-nucleobase conjugates for the inhibition of oncogenic miRNAs production

The discovery of new original scaffolds for selective RNA targeting is one of the main challenges of current medicinal chemistry since therapeutically relevant RNAs represent potential targets for a number...

Overview of the Structure, Side Effects, and Activity Assays of L-asparaginase as a Therapy Drug of Acute Lymphoblastic Leukemia

L-asparaginase (L-ASNase is abbreviation, L-asparagine aminohydrolase, E.C.3.5.1.1) is an enzyme that is clinically employed as an antitumor agent for the treatment of acute lymphoblastic leukemia (ALL). Although L-ASNase is known...

Comprehensive analysis of commercial fragment libraries

Screening of fragment libraries is a valuable approach to the drug discovery process. The quality of the library is one of the keys to success, and more particularly the design...

Antibacterial activities of plant-derived xanthones

The increasing threat to global health posed by antibiotic resistance remains a serious concern. This troublesome scenario has steered a need for the discovery and evaluation of novel antibacterial agents....

Recent advances in the discovery of protein tyrosine phosphatase SHP2 inhibitors

Src homology 2 domain-containing protein tyrosine phosphatase (SHP2) is a non-receptor protein tyrosine phosphatase encoded by the Ptpn11 gene, which regulates cell growth, differentiation and apoptosis via modulating various signaling...