Curcumin, a widely utilized flavor and coloring agent in food, has been shown to demonstrate powerful antioxidant, antitumor promoting and anti-inflammatory properties in vitro and in vivo. In the present work, synthesis of new heterocyclic derivatives based on Curcumin was studied. Compound 3 was synthesized via the reaction of furochromone carbaldehyde (1) with Curcumin (2) using pipredine as catalyst. Also, novel, 4,9-dimethoxy-5H-furo [3, 2-g] chromen-5-one derivatives 4a–d, 6a–d, 7, 8a–d, 9 and 10 were synthesized by the reactions of furochromone carbaldehyde (1) with different reagents (namely: appropriate amine 3a–d, appropriate hydrazine 5a–d, hydroxylamine hydrochloride, urea/thiourea, malononitrile, malononitrile with hydrazine hydrate). The structure of the synthesized products had been confirmed from their spectroscopic data (IR, ¹H-NMR, ¹³C-NMR and mass spectra). In the present investigation, the newly synthesized products were screened using the MTT colorimetric assay for their in vitro inhibition capacity in two human cancer cell lines (hepatocellular carcinoma (HEPG2) and breast cancer (MCF-7) as well as the normal cell line (human normal melanocyte, HFB4) in comparison to the known anticancer drugs: 5-flurouracil and doxorubicin. The anticancer activity results indicated that the synthesized products 4c and 8b showed growth inhibition activity against HEPG2 cell line and synthesized products 4b and 8a showed growth inhibition activity against MCF-7, but with varying intensities in comparison to the known anticancer drugs, 5-flurouracil and doxorubicin. Cyclin dependent kinase 2 (CDK2), a major cell cycle protein, was identified as a potential molecular target of Curcumin. Furthermore, Curcumin induced G1 cell cycle arrest, which is regulated by CDK2 in cancer cells. Therefore, we used molecular modelling to study in silico the possible inhibitory effect of CDK2 by Curcumin derivatives as a possible mechanism of these compounds as anticancer agents. The molecular docking study revealed that compounds 4b, 8a and 8b were the most effective compounds in inhibiting CDk2, and, this result was in agreement with cytotoxicity assay.

The current work was conducted to synthesize several novel anti-inflammatory quinazolines having sulfamerazine moieties as new 3CLpro, cPLA2, and sPLA2 inhibitors. The thioureido derivative 3 was formed when compound 2 was treated with sulfamerazine. Also, compound 3 was reacted with NH₂-NH₂ in ethanol to produce the N-aminoquinazoline derivative. Additionally, derivative 4 was reacted with 4-hydroxy-3-methoxybenzaldehyde, ethyl chloroacetate, and/or diethyl oxalate to produce quinazoline derivatives 5, 6, and 12, respectively. The results of the pharmacological study indicated that the synthesized 4–6 and 12 derivatives showed good 3CLpro, cPLA2, and sPLA2 inhibitory activity. The IC₅₀ values of the target compounds 4–6, and 12 against the SARS-CoV-2 main protease were 2.012, 3.68, 1.18, and 5.47 µM, respectively, whereas those of baicalein and ivermectin were 1.72 and 42.39 µM, respectively. The IC₅₀ values of the target compounds 4–6, and 12 against sPLA2 were 2.84, 2.73, 1.016, and 4.45 µM, respectively, whereas those of baicalein and ivermectin were 0.89 and 109.6 µM, respectively. The IC₅₀ values of the target compounds 4–6, and 12 against cPLA2 were 1.44, 2.08, 0.5, and 2.39 µM, respectively, whereas those of baicalein and ivermectin were 3.88 and 138.0 µM, respectively. Also, incubation of lung cells with LPS plus derivatives 4–6, and 12 caused a significant decrease in levels of sPLA2, cPLA2, IL-8, TNF-α, and NO. The inhibitory activity of the synthesized compounds was more pronounced compared to baicalein and ivermectin. In contrast to ivermectin and baicalein, bioinformatics investigations were carried out to establish the possible binding interactions between the newly synthesized compounds 2–6 and 12 and the active site of 3CLpro. Docking simulations were utilized to identify the binding affinity and binding mode of compounds 2–6 and 12 with the active sites of 3CLpro, sPLA2, and cPLA2 enzymes. Our findings demonstrated that all compounds had outstanding binding affinities, especially with the key amino acids of the target enzymes. These findings imply that compound 6 is a potential lead for the development of more effective SARS-CoV-2 Mpro inhibitors and anti-COVID-19 quinazoline derivative-based drugs. Compound 6 was shown to have more antiviral activity than baicalein and against 3CLpro. Furthermore, the IC₅₀ value of ivermectin against the SARS-CoV-2 main protease was revealed to be 42.39 µM, indicating that it has low effectiveness.

A new series of chalcones 4a-i; 6a,b, and 8 was synthesized from the condensation of ketone 2, which was prepared from the reaction of thiourea derivative 1 with 3- chloropentane-2,4-dione in MeOH at reflux temperature, with substituted aromatic/ heterocycle aldehydes in EtOH containing NaOH at room temperature. Antimicrobial and antioxidant activities were assessed for the synthesized compounds. The antimicrobial susceptibility tests revealed that compounds (4c, 4e, 4f, and 4i) exhibited good to excellent activity against C. albicans, S. aureus ATCC25923, E. faecalis ATCC29212, P. aeruginosa ATCC10145, and S. mutans ATCC25175. The antioxidant capabilities were assessed using the DPPH and ABTS radical scavenging methods. Compounds (4b, 4c, 4d, and 4e) proved to be better at scavenging DPPH and ABTS. This study involved in-silico drug-likeness and physicochemical properties and evaluated their ADMET profiles. According to the results of the molecular docking simulation, the synthesized compounds showed lower binding energy at the active sites of Dihydropteroate synthase, Sortase A, LasR, and Penicillin-binding protein pockets, which suggests that they may have an inhibitory effect on the enzymes and show promise as antimicrobial agents.

The focus of this review is on the synthetic routes available for different types of pyrazoloquinoline derivatives. There are three types of synthetic methods: i) from pyrazole derivatives; ii) from quinoline derivatives; and iii) miscellaneous methods. The position of the linkage between pyrazole and quinoline rings determines the seven isomers of pyrazoloquinolines. The purpose of this review is to provide a guide for both synthetic and medicinal chemists to discover and design new pyrazoloquinolines for medical purposes.

The gibbsite bearing shale occurrence in the Paleozoic sedimentary sequence of SW Sinai, Egypt, was found to be associated with several metal values. From sulfate liquor prepared by proper leaching, the recovery of these metal values has been studied. Alumina was first separated in the form of potash alum followed by Cu-selective extraction by hydroxyoxime LIX-973N solvent. Then U recovery using an anionic exchange resin Amberlite IRA-400 was achieved. For the associated heavy metal Zn, it was subsequently extracted using di-2-ethylhexyl phosphoric acid. The relevant factors affecting the extraction process were adequately studied

Introduction: Benzochromenes are heterocyclic compounds of growing interest in medicinal chemistry due to their diverse biological activities, including antioxidant, anticancer, and antimicrobial properties. Methods: A one-pot, three-component synthesis was employed to prepare benzochromene derivatives (4a–f) using 2-naphthol or its derivatives, active methylene compounds, and 2-methoxybenzaldehyde in ethanol with piperidine as a catalyst. The compounds were evaluated for their anticancer activity against MCF-7, HepG-2, and HCT-116 cell lines, as well as for their antimicrobial activity through molecular docking studies targeting cancerrelated and microbial proteins. Results: All synthesized compounds were obtained in moderate to good yields. Compounds 4c, 4e, and 4f demonstrated superior biological activity compared to standard drugs Doxorubicin and Augmentin. Docking studies revealed strong binding affinities to key targets, including the TGF-βI receptor and the choline-binding domain. Discussion: The hydroxyl group at position 9 in compounds 4c and 4f likely contributed to enhanced antimicrobial activity, while the bromo group in 4e correlated with significant anticancer effects. These findings suggest meaningful structure–activity relationships and validate the design strategy. Conclusion: The synthesized benzochromene derivatives exhibit promising anticancer and antimicrobial activities. Supported by molecular docking, these findings lay the groundwork for further pharmacological and in vivo evaluations of this scaffold.