Quinolyl-Based PGM Metallarectangles: Antiproliferative Activity,DNA and BSA Protein Interactions,and a Molecular Docking Perspective

The increased success of small metal-containing molecules as pharmaceutical agents has prompted investigations into the pharmacological activity of a different class of metal-based compounds; supramolecular coordination complexes (SCCs). Such complexes have been extensively investigated for their anticancer activity, with many displaying activities comparable or superior to available clinical chemotherapeutic drugs. Here, we evaluated a series of quinoline-containing binuclear complexes and metallarectangles for their in vitro anticancer activity in the hormone receptor positive MCF-7 and triple negative MDA-MB-231 breast cancer cell lines. The preliminary cytotoxic screen, in the MCF-7 cell line, revealed that the ligand (7-chloro-4-(pyridin-4-yl)quinoline, L ) and metallarectangle [{Ir(μ-Cl)(Cp*)}₄(μ- L )₂](OTf)₄ display superior activity to cisplatin, while [{Ru(p-cymene)}₄(μ-η²-η²-C₂O₄)₂(μ- L )₂](OTf)₄ was more potent than cisplatin in the triple-negative MDA-MD-231 cell line. Upon evaluation in a multidose screen, ligand L and metallarectangle [{Ir(μ-Cl)(Cp*)}₄(μ- L )₂](OTf)₄ displayed antiproliferative activity almost two-fold greater than cisplatin in the MCF-7 cell line, while [{Ru(p-cymene)}₄(μ-η²-η²-C₂O₄)₂(μ- L )₂](OTf)₄ was over two-times more active than cisplatin in the MDA-MB-231 cell line. Additionally, using the non-tumorigenic MCF-12 A breast epithelial cell line, the compounds demonstrate increased selectivity toward breast cancer cells over non-tumorigenic cells. Furthermore, investigations into the interactions of ligand L and selected complexes with calf thymus DNA (CT-DNA) and bovine serum albumin (BSA) indicate favourable binding.     

2-Amino-4-aryl-5-oxo-4,5-dihydropyrano[3,2-c]chromene-3-carbonitriles with Microtubule-Disruptive,Centrosome-Declustering,and Antiangiogenic Effects in vitro and in vivo

A series of fifteen 2-amino-4-aryl-5-oxo-4,5-dihydropyrano[3,2-c]chromene-3-carbonitriles ( 1 a – o ) were synthesized via a three-component reaction of 4-hydroxycoumarin, malononitrile, and diversely substituted benzaldehydes or pyridine carbaldehydes. The compounds were tested for anticancer activities against a panel of eight human tumor cell lines. A few derivatives with high antiproliferative activities and different cancer cell specificity were identified and investigated for their modes of action. They led to microtubule disruption, centrosome de-clustering and G2/M cell cycle arrest in 518 A2 melanoma cells. They also showed anti-angiogenic effects in vitro and in vivo.     

In vitro anticancer activity and comparative green synthesis of ZnO/Ag nanoparticles by moringa oleifera,mentha piperita,and citrus lemon

This study proposes a simple, effective, and environmentally friendly approach for the synthesis of zinc oxide/silver nanoparticles (ZnO/Ag NPs) using three different plant extracts. The plants used in this study were moringa oleifera (MO), mentha piperita (MP), and citrus lemon (CL). Characterizations of ZnO/Ag NPs were done using ultraviolet–visible spectroscopy (UV vis), X-ray diffraction (XRD), field emission scanning electron microscope (FESEM) along with energy dispersive spectroscopy (EDX), and fourier transform infrared spectroscopy (FTIR). In accordance with size distribution findings, ZnO/Ag NPs synthesized with MO have a narrow size distribution, with the average particle size being 119 ± 36 nm. Among these three reducing agent MO act as the best reducing agent. Moreover, the anticancer activity of silver nanoparticles (Ag NPs), zinc oxide nanoparticles (ZnO NPs) and ZnO/Ag NPs synthesized with MO were demonstrated in human cervical cancer cells (HeLA). The results revealed that ZnO/Ag NPs demonstrate in vitro cell viability of 72%, 81%, and 84% using 2.5, 5, and 10 μgml^?1of ZnO/Ag NPs for 24 h. While Ag NPs and ZnO NPs prepared with MO showed 50% and 60% cell viability using 2.5 μgml^?1concentration for 24 h. This showed that the ZnO/Ag NPs act as a strong anticancer agent compared to Ag NPs and ZnO NPs. Overall, this research proposes a green synthesis approach for ZnO/Ag NPs with a wide range of potential uses, particularly in biomedicine.     

Contribution of Knoevenagel Condensation Products toward the Development of Anticancer Agents: An Updated Review

Knoevenagel condensation is an entrenched, prevailing, prominent arsenal following greener principles in the generation of α, β-unsaturated ketones/carboxylic acids by involving carbonyl functionalities and active methylenes. This reaction has proved to be a major driving force in many multicomponent reactions indicating the prolific utility toward the development of biologically fascinating molecules. This eminent reaction was acclimatised on different pharmacophoric aldehydes (benzimidazole, β-carboline, phenanthrene, indole, imidazothiadiazole, pyrazole etc.) and active methylenes (oxindole, barbituric acid, Meldrum's acid, thiazolidinedione etc.) to generate the library of chemical compounds. Their potential was also explicit to understand the significance of functionalities involved, which thereby evoke further developments in drug discovery. Furthermore, most of these reaction products exhibited remarkable anticancer activity in nanomolar to micromolar ranges by targeting different cancer targets like DNA, microtubules, Topo-I/II, and kinases (PIM, PARP, NMP, p300/CBP) etc. This review underscores the efficiency of the Knoevenagel condensation explored in the past six-year to generate molecules of pharmacological interest, predominantly toward cancer. The present review also provides the aspects of structure-activity relationships, mode of action and docking study with possible interaction with the target protein.     

Evaluation of physicochemical and biological properties of SnO2 and Fe doped SnO2 nanoparticles

In recent decades, nanoparticle synthesis has been used for various physical and chemical methods. However, different toxic chemicals are used during this synthesis process to address these concerns, which has multiple effects on environmental toxicity and high cost. To avoid these problems, we need a cost-effective and environmentally friendly approach. In this study, green synthesis was used to make tin oxide (SnO₂) and ferrous doped tin oxide (SFO) nanoparticles (NPs) from Morinda citrifolia leaf extracts. The X-ray diffraction patterns of SnO₂ and SFO NPs reveal a tetragonal crystalline structure. From the FESEM image of synthesized SnO₂ and SFO NPs, their spherical structure and chemical composition were identified by EDX spectrum. Through the DLS spectrum, the hydrodynamic size was observed at 66 and 61 nm for SnO₂ and SFO NPs, respectively. In the FTIR spectrum, the O–Sn–O stretching vibration peak arises at (606 & 509 cm^?1 for SnO₂ NPs) and (613 & 538 cm^?1 for SFO NPs). Photoluminescence is used in materials to detect surface defects and impurity levels. The antibacterial activity of the SnO₂, SFO NPs, and conventional antibiotics like amoxicillin NPs is effectively inhibited against S. aureus and E. coli bacterial strains. SFO NPs exhibit a higher antibacterial activity as compared to SnO₂ and amoxicillin. The anticancer efficacy of increased SFO NPs compared to SnO₂ NPs was tested against (MDA-MB-237) human breast cancer cells. These results suggest that Fe ions modified SnO2 NPs could be used in healthcare industrial applications to improve human health.