Fullerene-Tetrabenzofluorene (C60-TBF) in Multivalent Photosensitisation for Enhanced ZnO-based Photo-catalysts: Mono vs. Hexakis Adduct

Photo-catalysts offer a simple catalytic method with widespread applications like degradation of polluting dyes, hydrogen generation from water, etc., in the presence of a photon source like sunlight. The development of a second-generation photo-catalyst in the form of a nanocomposite is an integral part of research to improve the practical usefulness and efficiency of the process. A systematic study using the active material with controlled functional groups is required to understand the process in detail as well as to develop efficient photocatalytic systems. In this paper, we report the design, synthesis, detailed physicochemical studies, and self-assembly of interesting materials where fullerenes have been functionalized with polycyclic, aromatic, conjugated, butterfly-shaped molecules like Tetrabenzofluorene (TBF) using a well-known click chemistry approach. Detailed analyses using spectroscopic, electrochemical, and microscopic or X-ray diffraction (single crystal) techniques were undertaken for a clear understanding of their photophysical or self-assembly behavior. The functionalized fullerene material was mainly used so that comparative results could be presented where two units (mono adduct) or twelve units (hexakis adduct) of TBF molecules were attached separately. These comparative studies were beneficial for unambiguous interpretation of results and drawing definitive conclusions regarding the energy transfer with cascade-type systems. Finally, those results were useful for the logical understanding of photo-catalytic experiments using those designer fullerene materials.

Design, Synthesis, and Characterization of Novel Series of Pharmacologically-important Sperm-shaped Amphiphilic Heterocyclic Compounds derived from Natural Palmitic Acid

Natural palmitic acid is a pivotal saturated fatty acid used in many biochemical processes occurring in humans and diverse living creatures, as it is the most common natural long-chain carboxylic acid whose unrivaled amphiphilic sperm-like skeleton with the inert single 15-C aliphatic chain (tail or carrier) and the very active one carboxyl group (head) represent a rich reactive entity and carrier for several organic/medicinal chemistry and pharmaceutics applications with respect to drug design and formulation. Derivatives of 1,3,4-oxadiazoles along with their 1,3,4-thiadiazoles and 1,2,4-triazoles analogs exhibit a broad spectrum of substantial pharmacological activities. Agreeing with the well-known hybridization principles and incorporation norms in hybrid chemistry, if a substituted nitrogenous heterocyclic aromatic nucleus of the three aforementioned kinds is straightway attached to the simple straight palmitic acid backbone at the position of the carboxyl group, the produced molecules are supposed to be very bioactive. This research work reports for the first once the efficient design/synthesis and characterization/elucidation of four one-tailed nitrogen-containing heterocyclic derivatives of palmitic acid constructure, which introduce a novel biologically-important pharmacophore having biocompatible amphiphilic sperm-shaped heteroaromatic structure.

Design, Synthesis of Amide Derivatives of Scutellarin And Their Anti-Leukemia And Neuroprotective Activities

A unique series of amide-scutellarin derivatives were designed and synthesized in order to develop the function of scutellarin further. The antiproliferative activity of all target compounds against two human leukaemia cell lines were evaluated. Among them, compounds 6g and 7c displayed the most antitumor activities against HL-60 and THP-1. Moreover, all compounds were also assayed for their neuroprotective activity against hydrogen peroxide (H2O2)-induced PC-12 cell injury, and the majority of the compounds had moderate to good neuroprotective properties. These findings confirmed that these target compounds could be used as anti-leukaemia and neuroprotective candicates in the future.

Design, Synthesis, Biological Evaluation and Molecular Docking Studies of 5-fluorouracil-dithiocarbamate Conjugates

In this paper, a series of novel 5-fluorouracil-dithiocarbamate conjugates were designed, synthesized and evaluated in vitro . The results of cytotoxicity assays illuminated that these conjugates had anti-tumor activity against B16, Hela and U87MG, and compound P3 exhibited excellent growth inhibition against U87MG cells. Interestingly, the cytotoxicity of these conjugates was significantly increased when combined with copper ions. Meanwhile, colony-formation assays, transwell migration assays, cell apoptosis assays and cell cycle distribution assays were performed to explore the anti-tumor mechanism of conjugates. Compound P3 and P4 exhibited good biological activity in above four experiments when combined with copper ions. Especially, P3 displayed better bioactivity compared to the other three compounds. These results indicated that conjugates might be metabolized in the cells to produce dithiocarbamates, then metabolites formed complexes with copper ions, generating anti-tumor effects. Furthermore, conjugates and their metabolized dithiocarbamate derivatives were investigated by molecular docking, the results exhibited that P3 had the strongest interaction with the proteins 6CCY and 5T92, which was consistent with the obtained results of cell experiments. Compound P3 might be a potential lead-compound for the treatment of breast cancer and glioma. Further research in vivo about these compounds would be performed in our following work.