Abstract: 1,4-dihydropyridine is a versatile class of compounds with multiple biological activities, thus holding significant pharmacological potential. Recent studies have provided evidence concerning the anticancer, antimicrobial, and anti-inflammatory properties of 1,4-dihydropyridines, as well as their potential in Alzheimer’s disease treatment. Therefore, this class of compounds is a promising candidate in studies of drug development and drug discovery. The major derivatives of 1,4-dihydropyridine can be synthesized through onepot synthesis in many different ways, varying the solvents, catalysts, and experimental conditions. Due to the compound’s remarkable potential and ease of production, in this review we aimed to present the biological activities and synthesis methodologies of the main 1,4-dihydropyridine derivatives reported by scientific literature over the past decade.

Abstract: In ethanolic piperidine solution, the interaction of 6-bromonaphthalen-2-ol (1) with α- cyano-p-chlorocinnamonitrile (2a) or ethyl α-cyano-p-chlorocinnamate (2b) yielded 4Hnaphtho[ 2,1-b]pyran-3-carbonitrile (3a) and 4H-naphtho[2,1-b]pyran-3-carboxylate (3b). The naphthopyran derivatives (3a, b) reacted with electrophilic reagents afforded naphthopyranopyrimidines and naphthopyrano-triazolopyrimidine derivatives. The structures of the newly synthesized compounds are confirmed through spectral analysis using NMR, IR, and MS spectroscopy. The anticancer efficacy of all compounds was investigated against three cancer cell lines: MCF- 7, HeLa, and PC-3, along with a molecular docking study.

Abstract: Rhodium catalysts for hydroformylation of aryl alkenes generally promote the formation of branched aldehydes. Here, we have demonstrated that by using a single rhodium catalyst containing a diphosphoramidite ligand derived from BINOL, it is possible to achieve the inversion of regioselectivity in the hydroformylation of aryl alkenes simply by reducing the syngas pressure or, alternatively, increasing the reaction temperature. Indeed, the hydroformylation of styrene carried out at 20 bar and 50°C resulted in 72% of 2- phenylpropanal, while at atmospheric pressure, 71% of 3-phenylpropanal was obtained. A similar linear selectivity (72-74%) was observed when the hydroformylation of styrene, pmethylstyrene, and p-methoxystyrene was performed at 10 bar and higher temperature (80°C). The regioselectivity of the hydroformylation of trans-β-methylstyrene under mild conditions (80°C, 10-20 bar) was also strongly influenced by the syngas pressure. The results of this study show that it is possible to reverse the selectivity of aryl alkenes hydroformylation with a single catalyst by simply exploring the reaction conditions. In this paper, we have shown that the inversion of the regioselectivity in the hydroformylation of aryl alkenes can be achieved using a single rhodium catalyst containing a BINOL-derived diphosphoramidite ligand by reducing the syngas pressure or, alternatively, increasing the reaction temperature.

Aim and Objective: To develop a ruthenium-catalyzed method to prepare meta-nitration containing 1,2,4-thiadiazoles with potential biological activity. Moreover, the current protocol should exhibit a relatively broad substrate scope and functional group compatibility. Materials and Methods: Materials and Methods: The best condition for the synthesis of nitration containing 1,2,4-thiadiazoles derivatives was carried out employing a mixture of 0.20 mmol of 1 (1a: 47.6 mg, 1b: 53.2 mg, 1c: 70.1 mg, 1d: 59.7 mg, 1e: 81.2 mg, 1f: 54.8 mg, 1g: 61.4 mg, 1h: 74.8 mg, 1i: 53.2 mg, 1j: 59.0 mg, 1k: 54.9 mg, 1l: 50.0 mg), Cu(NO3)2•3H2O (120.8 mg, 0.5 mmol), Ru3CO12 (9.6 mg, 7.5 mol %), TBAOAc (18.0 mg, 30 mol %), AgTFA (66.2 mg, 1.5 equiv), oxone (123.0 mg, 1.0 equiv), DCE (1.0 mL) placing in a Schlenk tube and stirred at 90 oC under air atmosphere for 36.0 h. Results: A series of 1,2,4-thiadiazoles containing compounds with potential biological activity were prepared in yield ranging from moderate to good under mild conditions, exhibiting a relatively broad substrate scope and functional group compatibility. Conclusion: We have developed a ruthenium-catalyzed 1,2,4-thiadiazoles-assisted regioselective meta-C-H nitration of arenes. This study provides a simple and efficient approach for synthesizing 1,2,4-thiadiazoles derivatives, yielding the nitration products in moderate to good yields. A mechanistic study indicated that a radical pathway might be involved in this transformation.

Abstract: Dess-Martin periodinane (DMP) is one of the hypervalent iodines that is most frequently utilized as an oxidizing agent in organic chemistry. The authors of this septennial review have critically and methodically presented representative applications of DMP in organic synthesis from 2015 to the present, including oxidations, dehydrogenations, hetero and homo-dimerizations, aromatizations, thiocyanations, halogenations, dearylations, ring expansions, cyclizations, heterocyclic ring formation, and other miscellaneous reactions. This review discusses the range and constraints of these transformations.

Abstract: Ruthenium-catalyzed olefin metathesis reactions were conducted in water with thermoresponsive block copolymers forming micelles. The block copolymers were prepared by living radical polymerization and consisted of a thermo-responsive and hydrophilic segments. The former segment included poly(N-isopropylacrylamide) or poly(N,N-diethylacrylamide), and the latter poly(sodium 4-styrene sulfonate), poly(sodium 2-acrylamido-2-methylpropanesulfonate) or poly(ethylene glycol). Homometathesis, cross-metathesis and ring-closing metathesis reactions proceeded to afford the products in moderate to good yields. Extraction efficiency from the reaction mixture was also studied.

Abstract: A new series of stilbene-arylcinnamide hybrids have been designed and synthesized with various substituents. These compounds were characterized by FTIR, 1D- and 2D-NMR as well as mass spectroscopy analysis (HRESIMS). The synthesized compounds were tested for their cytotoxic activity against human lung cancer A549 cell. The most active compound was further studied via in silico molecular docking on α,β- interface of tubulin. Total 18 new stilbene-arylcinnamide hybrids have been synthesized with 42-80% yield and evaluated for their cytotoxic activity against human lung cancer A549 cell. Particularly, compound 6b exhibited potent cytotoxicity against A549 cells with the IC50 value of 19.9 μM. In addition, compound 7b displayed moderate activities with the IC50 value of 33.9 μM, while other hybrids were considered inactive. Structural activity relationship (SAR) studies revealed that the presence of an isopropyl group at the para position on ring A and a methyl group at the para position on ring C is beneficial for enhanced cytotoxicity. Furthermore, we also developed an in silico molecular docking to study the binding interaction of the active compounds to the α,β-interface of tubulin (PDB ID: 3E22). Hybrids 6b and 7b demonstrated promising binding interactions and affinities into the tubulin active site with calculated binding energy of -7.2 and -8.0 kcal/mol, respectively.

Abstract: Hybrid molecules based on fullerene С60 and strained polycyclic hydrocarbons were synthesized for the first time using the Bingel–Hirsch reaction. The films of fullerene derivatives were deposited by centrifugation. The synthesized hybrid fullerene С60derivatives containing one strained polycyclic hydrocarbon moiety showed better charge carrier mobility than the fullerene derivatives containing two polycyclic hydrocarbon moieties. Apart from current–voltage characteristics, the morphology of the prepared hybrid compounds was studied. The best current– voltage characteristics were found for films with lower roughness. The fullerene С60 adducts containing strained polycyclic hydrocarbon moieties were used to fabricate organic field effect transistors (OFETs) with high-quality films; owing to this, the manufacturing process is compatible with modern printed organic electronics.

Abstract: Traditional Chinese medicine is an ancient system of wellness and health that has been used in almost all countries of the world, specially in Asia for thousands of years. : The growth, development, final yield and chemical compounds of medicinal plants can be negatively influenced by different kinds of biotic and abiotic stresses. Abiotic stress signals are chemical stress (Mineral salts, heavy metal, aerosols, gaseous toxins, pesticides, and pollutants), salinity (salt), temperature (Heat, cold), radiation (Ionisation radiation, light and UV), water (Flooding, drought) and mechanical stress (Submergence, wind, soil movement). Relevant literature has been obtained using the keywords “Traditional Chinese Medicine”, “Abiotic Stress”, “Biotic Stress”, “Ginseng”, “Ginger”, “Goji berry”, “Astragalus”, “Ginkgo”, “Artemisia annua L.”, “LC-MS”, “GC-MS”, and “NMR” in scientific information, namely “Web of Science”, “PubMed”, “SciFinder”, and “Elsevier”. Some of the plants’ secondary metabolites under different growth conditions are Camptothecin (Camptotheca acuminata), Capsaicin (Capsicum sp.), Rosmarinic acid (Salvia miltiorrhiza), Codeine (Papaver somniferum), Resveratrol (Grapes, groundnut), Artemisinin (Artemesia annua), Allicin (Allium sativum), Rohitukine (Dysoxylum binectariferum), Stevioside (Stevia rebaudiana), Andrographolide (Andrographis paniculata), Saikosaponins (Bupleurum chinense), Sennosides (Cassia augustifolia), Rutin (Dimorphandra mollis), Valepotriates (Valeria species), Indole alkaloids (Catharanthus roseous), and Furanocoumarins (Bituminaria bituminosa). : The aim of this article is a survey of active chemical compounds and metabolic changes of some of the most important medicinal plants in traditional Chinese medicine (TCM) in both abiotic and biotic stresses. : Future research is needed to evaluate the effects of biotic and abiotic stresses on chemical compounds and active metabolites of medicinal plants specially traditional Chinese medicine, and more surveys on the roles of LC-MS, GC-MS and NMR techniques for a better understanding of chemical components of medicinal plants.

Abstract: 5-Amino-4-formyl pyrazole 1 was used as a precursor for the synthesis of 6- aminopyrazolo[3,4-b]pyridine-5-carbonitrile 2, and 6-aminopyrazolo[3,4-b]pyridine-5- carboxamides 3 and 4. Pyrazolo[3,4-b]pyridines 2, 3, and 4 were treated with different reagents leading to structurally confirmed heterocycles. Mosquito adult females carry and transmit the causatives of many diseases to humans and other domestic animals. Therefore, their management has become a necessity. Ten of the synthesized compounds were tested for larvicidal activity against second-stage C. pipiens larvae. : IR spectra were recorded on Shimadzu-408 infrared spectrophotometer. The NMR spectra were performed on a Bruker AV-400 spectrometer and JEOL ECA II 500 MHz. Mass spectrometry was provided on a Varian MAT 312 instrument in EI mode (70 eV). Lethal concentrations were calculated based on probit analysis. Biochemical enzymes were analyzed using analysis of variance ANOVA with Graph Pad Prism 5. Mean comparisons were analyzed using Tukey's test. : Five compounds, 1, 2, 4, 5 and 11 exhibited detectable insecticidal activity as these compounds recorded 154.4, 5.6x103, 8.4, 135.1 and 697.2 ppm, respectively. Moreover, the effect of these insecticidal compounds on lipids and carbohydrates digestive pathways in the larvae was evaluated by comparing the activities of amylase and lipase digestive enzymes in both control and treated larvae. Compounds 1, 4 and 5 showed an inhibitory effect on both lipase and amylase enzymes. Compound 2 inhibited lipase activity, while compound 11 didn’t affect both enzymes compared with the control. : Results showed that the incorporation of pyridine and pyrazole induced significant insecticidal activity against larval mosquitoes. Furthermore, insertion of amino or carbonyl groups into the synthesized compounds enhanced the insecticidal activity. Our findings showed that development of such novel compounds is promising in enhancing the agricultural productivity and management of diseases transmitted by insects.