Synthesis of bioactive heterocycles using reusable heterogeneous catalyst HClO4–SiO2 under solvent-free conditions

We are reporting a simple, efficient and green protocol for the synthesis of chromenes and dihydropyrimidines (products of Knoevenagel and Biginelli reaction, respectively) by the use of silica-supported perchloric acid (HClO₄–SiO₂) as an effective heterogeneous catalyst. Short reaction times, high product yields, simple procedure and reusability of the catalyst are the superior characteristics of this protocol.     

Asymmetric ring-opening reaction of azabenzonorbornadienes with phenols promoted by palladium/(R,R)-DIOP complex

An efficient asymmetric ring opening reaction of azabenzonorbornadienes with various phenols using Palladium/(R,R)-DIOP complex has been demonstrated, the reaction afforded the corresponding products in excellent yields (80–95%) with moderate enantioselectivities (50–64% ees). The syn-configuration of the product was confirmed by the single X-ray crystallography.     

Regioselective Synthesis of Polyaza Pyrimidines and Polyaza Pyrazoles under One‐Pot Multicomponent Reaction Conditions

Convenient methods of synthesis of novel polyaza pyrimidines and polyaza pyrazoles have been described in this paper. The synthetic method is based on one‐pot, three‐component cyclocondensation of α‐oxoketene dithioacetals, 2,6‐diaminopyridine, and guanidine/hydrazine. Polyaza S,N‐acetals have been generated in situ by treating α‐oxoketene dithioacetals with 2,6‐diaminopyridine in the presence of n‐butyl lithium, which were subsequently treated with guanidine nitrate and hydrazine hydrate to afford polyaza pyrimidines and polyaza pyrazoles, respectively.     

Magnetic properties of Cr substituted Li–Sb ferrites

The magnetic properties, such as initial permeability and hysteresis loop properties of the chromium substituted Li–Sb ferrite system have been investigated. The SEM micrographs reveal the microstructure of the samples. The initial permeability is observed to decrease with the increase of chromium concentration. Frequency variation of permeability indicates that for all samples the resonance peak due to domain wall oscillations is at a frequency above 15 MHz. The hysteresis loop parameters have been calculated from the hysteresis loop studies. The magnetic parameters are observed to decrease with higher level of substitution.     

A f acile,regioselective synthesis of novel 3-( N-phenylc arbox amide)pyr azolo[1,5- a]pyrimidine an alogs in the presence of KHSO$$_{}$$ in aqueous medi a assisted by ultr asound and their antib acteri al activities

An environmentally benign, simple, efficient, and convenient route is described for the synthesis of novel pyrazolo[1,5-a]pyrimidine derivatives under ultrasound irradiation. Condensation of aminopyrazole 5 with formylated active proton compounds (6, 8, E–G, 12, and 15) furnished pyrazolopyrimidine (7, 9, 10, 13, and 16) in high-to-excellent yields. In comparison with conventional methods, ultrasound irradiation offers several advantages, such as shorter reaction time, higher yields, milder conditions, and environmental friendliness. The reaction is clean with excellent yields and reduces the use of solvents. X-ray crystallographic study of compound 7c confirmed the regioselectivity of the reaction. The antibacterial profile of the newly synthesized compounds was evaluated by cup and saucer method.     

Essential oil of Cephalotaxus griffithii needle inhibits proliferation and migration of human cervical cancer cells: involvement of mitochondria-initiated and death receptor-mediated apoptosis pathways

This study was conducted to determine the effect of Cephalotaxus griffithii needle essential oil (CGNO) on proliferation and migration of human cervical cancer (HCC) cells. CGNO treatment decreased the viability of all the tested HCC (HeLa, ME-180 and SiHa) cells. Morphological and DNA fragmentation analysis of CGNO-treated HeLa cells indicated the involvement of apoptosis in inducing HCC cell death. CGNO increased mitochondrial membrane depolarisation and upregulated the expression of caspase-9, caspase-8, caspase-3 and cleaved-PARP. The activity of caspase-8 and caspase-9 was also significantly increased. Wound healing and transwell migration assay demonstrated that CGNO significantly inhibited the migration of HeLa cells to close a scratched wound and also inhibited their migration through filter towards a chemotactic stimulus. Taken together, these results indicated that CGNO inhibited the proliferation and migration of HCC cells. Of note, CGNO induced HeLa cell death through mitochondria-initiated and death receptor-mediated apoptosis pathway.