Selective Recognition of c-KIT 1 G-Quadruplex by Structural Tuning of Heteroaromatic Scaffolds and Side Chains.

In this study, carbazole (MC) and dibenzofuran (MD) derivatives were synthesized to examine their effect on the biomolecular recognition of G-quadruplex (G4) targets. Biophysical studies revealed that MC-4, a carbazole derivative, exhibits a specific affinity and effectively stabilizes the c-KIT 1 G4. Molecular modeling suggests a stable interaction of MC-4 with the terminal G-tetrad of c-KIT 1 G4. Biological studies demonstrate that MC-4 efficiently enters cells, reduces c-KIT gene expression, and induces cell cycle arrest, DNA damage, and apoptosis in cancer cells. These findings demonstrate MC-4 as a selective c-KIT G4 ligand with therapeutic potential, providing insight into the structural basis of its anticancer mechanisms.

Cycloaddition of N-sulfonyl and N-sulfamoyl azides with alkynes in aqueous media for the selective synthesis of 1,2,3-triazoles.

The cycloaddition of N-sulfonyl and N-sulfamoyl azides with terminal alkynes generally produces amide derivatives via ketenimine intermediates. We herein delineate a Cu(I) catalyzed method using a prolinamide ligand that selectively generate N-sulfonyl and sulfamoyltriazoles in aqueous media by inhibiting the cleavage of the N1-N2 bond of 5-cuprated triazole intermediates. The present method is mild and tolerant to air, moisture and a wide range of functional groups thereby providing an easy access to a variety of triazole products.

Chemically synthesized butein and butin: Optical, structure and electrochemical redox functionality at electrode interface.

Progress in the development of phytochemistry has delivered advancement in materials functionality for range of inter/trans-disciplinary application. Here, we investigated the structural functionality of chemically synthesized phytoconstitutent, chalcone (butein) and flavanone (butin). Photoactive and electroactive behavior of butein and butin were comprehensively studied using UV-vis absorbance, photoluminescence and cyclic voltammetric techniques. Surface morphology of the butein and butin powders was characterized from scanning electron microscope at an operating voltage of 10 kV. Significant ultraviolet absorbance property are observed from butein and butin due to the distribution of π → π* and n → π* transitions. Photoluminescence emission spectra of the prepared materials are well resolved at visible region via keto-enol tautomerization and can be influenced by solvent pH. Cyclic voltammetric studies on the prepared materials enabled a direct electron-transfer reaction at gold-screen printed electrode, indicating the feasibility for analytical validation in herbal industries. Existence of multiple electroactive hydroxyl groups makes butein and butin a redox-functional species at electrode interface. Dispersion ability in aqueous and organic solvents makes butein and butin suitable for variety of photochemical applications. This phytochemical material offers new degrees of optical and redox functionality similar to inorganic nanostructures, in addition to inherent bioactivity, that may be advantageous for further biomedical function.