Synthesis and Anticancer Activity of 1,2,3-Triazole Fused N-Arylpyrazole Derivatives

A novel series of triazole derivatives 11a–11j is synthesized. Structures of the products are confirmed by ¹H and ¹³C NMR, and mass spectral data. The anticancer activities of compounds 11a–11j are evaluated against three human cancer cell lines (MCF-7, A549, and A375) using the standard MTT assay in vitro, using doxorubicin as the positive control. All the compounds exhibit significant activity against cancer cell lines. The compounds 11a, 11d, 11e, 11g, and 11j demonstrate more potent activity than the positive control.

     

Detailed investigation of a γ-cyclodextrin inclusion complex with l-thyroxine for improved pharmaceutical formulations

Thyroxine is a naturally occurring human hormone produced by the thyroid gland. Clinical applications of thyroxine to treat several chronic disorders are limited by poor water solubility and instability under physiological conditions. An inclusion complex of levo-thyroxine (l-thyroxine), the active form of the hormone with gamma cyclodextrin (γ-CD) has been obtained and studied with the aim of improving oral delivery rather than the injection formulation of the sodium salt. In addition to greater patient acceptability, inclusion complexes often improve aqueous solubility and bioavailability, stability, and reduce toxicity of drugs, thus providing enhanced pharmaceutical formulations. Physicochemical characterization of the inclusion complex was carried out using Fourier transform infrared spectroscopy, X-ray diffractometry, differential scanning calorimetry, scanning electron microscopy and proton nuclear magnetic resonance spectroscopy. Intermolecular dipolar interactions for the inclusion complex were also studied using 2 dimensional ROESY experiments. Formation of the inclusion complex between the protons H3 and H5 of cyclodextrin with aromatic protons of thyroxine was confirmed by their dipolar interaction. Molecular modelling was used to understand the basis for the complex formation and predict the formation of other complexes. Interestingly, we found that l-thyroxine forms an inclusion complex only with the larger γ-CD and not with other available alpha and beta forms.     

Photoactive barbiturate receptors: an ultimate lock-and-key system in which the key unlocks the lock

Conditional photofragmentation is achieved with binary systems incorporating the isophthaloyl bis-aminopyridine barbiturate recognition motif and dithiane- or trithiane-based photolabile modules, which cleave only in the presence of an external sensitizer. The components of the host-guest molecular recognition pair were each outfitted with either the sensitizer or the photocleavable module. In these pairs, photoinduced fragmentation is contingent on a molecular recognition event, which brings the sensitizer into the immediate proximity of the photolabile latch. [structure: see text]     

Usage of Platinum Nanoparticles for Anticancer Therapy over Last Decade: A Review

The quest for new functional nanomaterials is one of the defining purposes of nanoscience and nanotechnology. A large number of metal nanoparticles (NPs) are extensively exploited for biomedical applications. Metal NPs, in particular platinum NPs (PtNPs), possess remarkable properties that make them a potential candidate as a diagnostic or therapeutic agent. Due to potential technological interest over the last decade, PtNPs have attracted much attention in the field of anticancer research. PtNPs, when conjugated with many functionalizing agents such as polymers, ligands, drugs, peptides, and surfactants, exhibit improved targeting and reduced cytotoxic effects in various cancers. The PtNPs conjugated with folic acid, graphene oxide, and iron NPs are gained more attention due to their stability, large surface area, and reduced toxicity. To achieve this goal, PtNPs are co-loaded with drugs or other modalities that offer an opportunity for multimodal activity in the frame of treating cancer types focusing on breast, blood, lung, ovarian, skin, liver, etc. However, a review of PtNPs’ function in diagnosis and treatment is still lacking. In this review, the effectiveness of PtNPs toward inducing and elevating death of the cancerous cells proving its delivery approaches and antitumor nature, concluding with future perspectives, are summarized.