The Mizoroki-Heck reaction between in situ generated alkenes and aryl halides: cross-coupling route to substituted olefins.

This review covers palladium-catalyzed typical Mizoroki-Heck cross-coupling reactions of aryl halides with in situ generated alkenes, by following a typical Heck coupling mechanism to form substituted olefins unlike direct cross-coupling of alkenes with aryl halides in Heck olefination. These reactions solve the issue of alkenes undergoing polymerization at high temperatures and increase reaction efficiency by reducing the reaction time and purification steps.

Noscapine-Amino Acid Conjugates Suppress the Progression of Cancer Cells.

Lung cancer is the leading cause of cancer deaths globally; 1 in 16 people are diagnosed with lung cancer in their lifetime. Microtubules, a critical cytoskeletal assembly, have an essential role in cell division. Interference with the microtubule assembly leads to genetic instability during mitosis and cancer cell death. Currently, available antimitotic drugs such as vincas and taxanes are limited due to side effects such as alopecia, myelosuppression, and drug resistance. Noscapine, an opium alkaloid, is a tubulin-binding agent and can alter the microtubule assembly, causing cancer cell death. Amino acids are fundamental building blocks for protein synthesis, making them essential for the biosynthesis of cancer cells. However, the ability of amino acids in drug transportation has yet to be exploited in developing noscapine analogues as a potential drug candidate for cancer. Hence, in the present study, we have explored the ninth position of noscapine by introducing a hydroxymethylene group using the Blanc reaction and further coupled it with a series of amino acids to construct five target conjugates in good yields. The synthesized amino acid conjugate molecules were biologically evaluated against the A549 lung cancer cell line, among which the noscapine-tryptophan conjugate showed IC50 = 32 µM, as compared to noscapine alone (IC50 = 73 µM). Morphological changes in cancer cells, cell cycle arrest in the G1 phase, and ethidium bromide/acridine orange staining indicated promising anticancer properties. Molecular docking confirmed strong binding to tubulin, with a score of -41.47 kJ/mol with all 3D coordinates and significant involvement of molecular forces, including the hydrogen bonds and hydrophobic interactions. Molecular dynamics simulations demonstrated a stable binding of noscapine-tryptophan conjugate for a prolonged time (100 ns) with the involvement of free energy through the reaction coordinates analyses, solving the bioavailability of parent noscapine to the body.

Fabrication of Superparamagnetic Bimetallic Magnesium Nanoferrite Using Green Polyol: Characterization and Anticancer Analysis in Vitro on Lung Cancer Cell Line A549.

Magnetic bimetallic nanoparticles find many industrial and clinical applications in the field of water treatment, antibacterial and anticancer activities. Therefore, the current article reports green synthesis using oleo-polyol as a surface modifier and synthesis agent for bimetallic magnetic magnesium ferrite nanoparticles. The role of hydroxyl functionality of castor oil (a natural polyol) on the enhancement of structural, morphological, magnetic, and particle size properties has also been discussed. These properties were characterized using FTIR, XRD spectroscopy, SEM, AFM, and TEM microscopy, Brunauer-Emmett-Teller (BET), and vibrating sample magnetometer (VSM) techniques. The effect of calcination temperatures (600-900 °C) on particle size (23-40 nm to 500-600 nm), crystallite sizes (73.15-292.67 nm), and saturation magnetization (20.87, 23.07, 32.39, and 33.13 emu g-1) was analyzed. The influence of calcined temperatures on the anticancer activity of these nanoparticles has also been investigated in vitro using lung cancer cells (A549). Their biocompatibility, cytotoxicity, flow cytometry, and statistical analysis against lung cancer cells (A549) have been discussed. The green synthesis of magnesium nanoferrite particles using natural polyol and their application as anticancer agents against lung cancer cells (A549) have not been reported previously. They have exhibited far superior IC50 values and anticancer activity as compared to other reported metal oxides and magnesium oxide nanoparticles.

Metal catalyzed C-H functionalization on triazole rings.

The present review covers advancement in the area of C-H functionalization on triazole rings, by utilizing various substrates with palladium or copper as catalysts, and resulting in the development of various substituted 1,2,3- and 1,2,4-triazoles. Synthesis of these substituted compounds is necessary from the perspective of pharmaceutical, medicinal, and materials chemistry.

Use of gold nanoparticle-silibinin conjugates: A novel approach against lung cancer cells.

Lung cancer presents one of the most challenging carcinomas with meager 5-year survival rates (less than 20%), high metastasis and high recurrence due to chemo- and radio- resistance. An alternative or complementation to existing prognosis modalities is the use of phytochemicals such as silibinin, which targets essential cytokines, angiogenic factors and transcription factors for a profound anti-tumor effect. However, the problems of low solubility in an aqueous physiological environment, poor penetration, high metabolism and rapid systemic clearance limit the therapeutic use of silibinin. Conjugation of gold nanoparticles (GNPs) with silibinin may overcome the above challenges along with distinct advantages of biocompatibility, optical properties for monitoring and causation of cytotoxicity in cancer cells. The current study thus aims to develop silibinin conjugated gold nanoparticles (Sb-GNPs) with pH responsive release in the cancer microenvironment, optimizing several parameters for its higher activity and further evaluate the nanoplatform for their efficacy in inducing cell death in vitro against A549 lung cancer cells. GNPs was synthesized using trisodium citrate dihydrate as the reducing agent and further used for the conjugation of silibinin. The synthesized GNPs were found to be monodispersed and spherical in shape. The silibinin was successfully conjugated with gold nanoparticles and long-term stability of GNPs and Sb-GNPs nanoconjugates in suspension phase was confirmed by FTIR and DLS. Anticancer properties of Sb-GNPs were confirmed by different assay using MTT, Trypan blue dye exclusion assay and cell cycle analysis assay. After conjugation of silibinin with GNPs, the efficacy of silibinin increased 4-5 times in killing the cancer cells. This is the first report on using silibinin gold nanoconjugate system for lung cancer therapy with promising future applications.