Mini Reviews in Medicinal Chemistry - Online First

This review delves into the potential of nanotechnology for improved lung cancer diagnosis and treatment. A critical focus is placed on various overexpressed biomarkers within lung tumors. These biomarkers serve as potential targets for nanoparticle-based drug delivery strategies. The review explores two main targeting approaches: passive and active (receptor-based) targeting. Active targeting mechanisms like EGFR, folic acid, and CD44 receptor targeting are specifically discussed. Additionally, the review examines stimuli-responsive systems for targeted drug delivery, including pH, temperature, ligand-attached, and multi-stimuli-responsive systems. Moreover, the role of nanotechnology in theranostics, which combines therapeutic and diagnostic capabilities, is explored and different types of nanocarriers, including lipid-based, polymer-based, metal-based, and magnetic nanoparticles, are examined for their potential applications. The review also highlights advancements in lung cancer diagnostic techniques beyond nanotechnology. This includes emerging tools like biomarkers, biosensors, and artificial intelligence, alongside improvements to established methods. Finally, the review provides a glimpse into ongoing clinical trials and concludes by emphasizing the transformative potential of nanotechnology in improving lung cancer patient outcomes.

Currently, the synthesis of bioactive sulfonamides using amino acid as a starting reagent has become an area of research interest in organic chemistry. Over the years, an amine-sulfonyl chloride reaction has been adopted as a common step in traditional sulfonamide synthetic methods. However, recent developments have shown amino acids to be better precursors than amines in the synthesis of sulfonamides. Although amines and amino acids have some structural similarities, using amino acids rather than amines in the synthesis of sulfonamides minimizes several drawbacks. Comparatively, amino acids are preferred to amines as starting reagents in sulfonamide synthesis due to their biological relevance, chirality, stereochemistry, diversity of side chains, orthogonality in functional group manipulation, the potential for peptide and protein synthesis, mild reaction conditions, alignment with green chemistry principles, diverse synthetic applications, easy availability, and economic viability. Amino acids, having the aforementioned properties, offer a versatile platform for the synthesis of sulfonamides with tailored structures. The reaction mechanism of the synthesis of amino acid-derived sulfonamides involves a nucleophilic attack by the amino group on the activated sulfonyl species to produce a sulfonamide functional group. Amino acid-based sulfonamides have numerous pharmacological activities, including antibacterial, antiviral, anticancer, antioxidant, anti-inflammatory, anti-plasmodial, antimalarial, anti-trypanosomal, and insect growth regulatory properties. This review discusses several synthetic processes, emphasizing established ways, cutting-edge techniques, and novel approaches that emphasize the significance of amino acids in the synthesis of sulfonamides. The structure-activity relationship of amino acid-derived sulfonamides and their pharmacological activities are also highlighted.

Carbamate has been extensively used as a scaffold in the recent era of drug discovery and is a common structural motif of many approved drugs. The carbamate moiety's unique amide-ester hybrid (-O-CO-NH-) feature offers the designing of specific drug-target interactions. Despite the discovery of numerous carbamate derivatives that act on the endocannabinoid system (ECS), the development of clinically effective carbamates remains a challenge. In this review, we highlight the therapeutic potential of carbamate inhibitors of endocannabinoid degrading enzymes as a breakthrough in discovering neurotherapeutic drugs. We discuss the design strategies and medicinal chemistry aspects involved in developing carbamate-based molecular architectures that modulate the endocannabinoid signaling pathway by interfering with fatty acid amide hydrolase (FAAH), monoacylglycerol lipase (MAGL), and α/β-Hydrolase domain-containing 6 (ABHD6). Additionally, we highlight the dual activity profile of carbamates against FAAH and MAGL, FAAH and cholinesterase, and FAAH and TRPV1 channels. Furthermore, we illustrate the pharmacophores of O-functionalized carbamates and N-cyclic carbamates that are crucial for FAAH and MAGL inhibitory activities, respectively.