Pladienolide B (1), a macrocyclic polyketide isolated from Streptomyces platensis Mer-11107, displays potent antiproliferative and antitumor activities through its interaction with the SF3b subunit of the spliceosome. Herein, we report a divergent, s...
The incorporation of ferrocene into established pharmacophores represents a promising strategy for combining targeted activity with the properties of the organometallic scaffold. Building on our previous work on ferrocene-modified tyrosine kinase inh...
Urolithin M7 is a gut microbial metabolite of ellagic acid, but its glucuronide conjugate has not been well characterized. We report the first total synthesis of urolithin M7 3-glucuronide through a convergent route that combines Pd-mediated intramol...
A series of five novel 3-methyl-1-phenyl-4-(4-thioaroyl)-pyrazol-5-ones is obtained in excellent yields by thionation of the corresponding O-analogues with Lawesson’s reagent. The products are characterized in solution and solid phase. It is fo...
Catalysis has been recognized as a key science in contemporary chemistry, owing to the significant potential of nanocatalysts and organic–inorganic hybrid materials, due to their high surface area and tunability properties, as well as the possi...
The influence of the counter anion and solvent on the N-heterocyclic carbene (NHC)-catalyzed nucleophilic aroylation of electron-deficient aromatic compounds was investigated using iodide, bis(trifluoromethanesulfonyl)imide (TFSA), and tetrafluorobor...
The amide macrocyclic complexes of zinc [ZnMc1, ZnMc2, and ZnMc3 (1–3)] were synthesized through template condensation of oxalic acid with different diamines, p-phenylenediamine, ethylenediamine, and propylenediamine, respectively. These zinc c...
Six ortho-substituted halogen derivatives (F, Cl, Br) of mono- and analog bisthiocarbohydrazones were synthesized and fully characterized. Structural characterization was performed through elemental analysis and NMR, FT-IR and UV-Vis spectroscopy. Al...
The development of environmentally sustainable synthetic approaches for biologically active heterocyclic compounds has become increasingly important in medicinal chemistry. In this study, two dihydropyrimidinone (DHPM) derivatives were synthesized th...
Betulin, a lupane-type pentacyclic triterpene abundant in birch bark, is an accessible renewable scaffold for semisynthetic chemistry, while its 3,28-diacetate serves both as an isolable derivative and as a protected intermediate for further function...
The increasing prevalence of antimicrobial resistance has stimulated interest in non-antibiotic small molecules that can restore or potentiate the activity of established antibacterial agents. In this study, a focused series of low-molecular-weight c...
East Asian crowberry has been reported under Empetrum nigrum var. japonicum and E. nigrum subsp. asiaticum. This critical narrative review evaluates taxonomy, phytochemistry, and pharmacological evidence from Korean, Japanese, and Chinese source-repo...
Indolo[2,3-b]quinoxalines and their N-substituted derivatives exhibit anticancer activity. In this work, a convenient two-step protocol comprising base-promoted aldol condensation followed by oximation was used for the synthesis of novel β-hydro...
The development of sustainable and efficient methods for carbon–carbon (C–C) bond formation remains the main objective in modern organic synthesis. In recent years, photocatalysis has developed as a suitable alternative to conventional tr...
Active molecules derived from traditional Chinese medicine (TCM) represent a valuable source of lead compounds for modern drug discovery, demonstrating considerable potential in the prevention and treatment of chronic diseases, cancer therapy, and im...
Fluorinated isoquinoline-1,3-diones possess important biological activities and application value in many fields such as medicine, pesticides, and organic synthesis. This review summarizes the synthetic methods of fluorinated isoquinoline-1,3-diones...
The consistent increase in atmospheric CO2 concentration, mostly driven by the global combustion of fossil fuels, is considered one of the primary contributors to the increasing severity of environmental problems, like climate change and global warmi...
Flexible organic solar cells (FOSCs) are a promising green energy technology due to their mechanical flexibility, light weight, low cost, and compatibility with large-area solution processing. Although the power conversion efficiency (PCE) of rigid o...
Due to the rapid development of the textile industry and increased consumption of various textiles composed of both synthetic and natural fibers, large amounts of textile waste are produced, leading to environmental and economic problems on a global...
Pancreatic ductal adenocarcinoma (PDAC) is considered as one of the most lethal malignancies, characterized by late diagnosis, aggressive local invasion, profound therapy resistance, and a suppressive tumor microenvironment. Currently known chemother...
Ring-closing carbonyl-olefin metathesis (COM) reactions provide a straightforward method for producing cyclic alkenes from precursors containing carbonyl functional groups tethered to nucleophilic alkenes. Within the last decade, many methods for car...
We have prepared two novel tethered (arene)Ru(II)/TsDPEN complexes, one containing a p-OTBS on the η6-arene ring, and the other with a p-CO2Et group at the same position, representing an electron-rich and electron-poor derivative. These have been...
Phenylglycine (Phg) is a nonproteinogenic α-amino acid found in various bioactive molecules. The C-terminal activation of N-acyl Phg is often accompanied by oxazolone-mediated racemization, arising from the direct attachment of the phenyl ring...
Ninhydrins represent a promising chemical space for the search for new biologically active molecules with antimicrobial, antiprotease, and antitumor properties. In the present work, new ninhydrin derivatives were synthesized, and for the first time,...
Our recent studies demonstrated that dialkylaminopyridine organocatalysts featuring an extensive secondary sphere preferentially phosphorylate the alcohol at the apolar domain of a model amphiphilic diol. In the present study, this site-selective beh...
We report the synthesis and single-crystal X-ray structures of three novel (Z)-5-arylidene-3-phenylrhodanine derivatives, differing in the substituents on the benzylidene fragment (two methoxy groups (compound I), a dioxine ring (compound II), or a d...
Conventional oxidative hair dyes rely on aromatic amines, raising concerns about human health and environmental safety. This study reports a natural hair-coloring system using size-controlled ink particles (SIPs, ~170 nm in diameter) from cuttlefish...
1,2,4-Trisubstituted chiral homoallylic alcohols are valuable intermediates in natural product synthesis and complex molecular architectures; however, their catalytic asymmetric synthesis remains challenging due to the need for precise control of reg...
This study presents a theoretical investigation of the adsorption and electronic structure of two imidazole derivatives, 4-(1,4,5-triphenylimidazol-2-yl)-aniline (M1) and N,N-dimethyl-4-(1,4,5-triphenylimidazol-2-yl)-aniline (M2), on an Fe(100) surfa...
Reaction of 5-oxo-1-(4-(phenylamino)phenyl)pyrrolidine-3-carbohydrazide with selected aldehydes and ketone provided novel hydrazone derivatives bearing azole moieties: pyrazole, pyrrole, and indole. The drug likeness of the newly synthesized compound...
Thiocarbohydrazone derivatives represent a highly significant class in medicinal chemistry, characterized by a versatile scaffold defined with a thiocarbonyl (C=S) core and one or two imine (–C=N–) functionalities, allowing for precise mo...
We synthesized two vitamin D3 analogues, 3 and 4, which have a shortened or elongated fluoro-side-chain based on 24,24-difluoro-25-hydroxyvitamin D3 (5) using an efficient convergent approach and studied their preliminary biological activity. Both an...
This work presents a revised total synthesis of two pharmacologically relevant benzofurans using newly developed environmentally friendly methodologies. In particular, we focused on establishing improved synthetic routes to stilbene dimers under mild...
Aloe-emodin is an anthraquinone with a wide range of medicinal applications, including anti-angiogenic, anticancer, antimicrobial, antiviral, anti-inflammatory, and antioxidant activities. In this review, the functionalization of aloe-emodin using va...
A new series of eight novel etodolac-based 1,3,4-oxadiazoles was synthesized, characterized, and tested in silico in multidimensional routes, starting with etodolac, a well-known nonsteroidal anti-inflammatory medication (NSAID). In silico studies we...
Salophen-type Schiff base ligands derived from salicylaldehyde and naphthalene aldehydes were synthesized and coordinated to Ni(II) to obtain three nickel complexes (NiL1–NiL3), which were evaluated as heterogeneous electrocatalysts for the met...
The study aimed to verify the possible use of DFT calculation in the prediction of the orientation in electrophilic aromatic substitution. An activated ortho/para orienting substrate, and a deactivated meta orienting substrate, were used in DFT calcu...
In the present work, we describe the synthesis of a new heterocyclic derivative, 2-(naphthalen-1-yl)-2,3,5,6-tetrahydro-1H-isoquinolino[8,1,2-hij]quinazoline 1, using the reaction between the aminal 1,3,6,8-tetraazatricyclo[4.4.1.13,8]dodecane 2 (TAT...
2-Aryl-2-(3-indolyl)acetohydroxamic acids have emerged as promising antitumor agents; however, their poor pharmacokinetic profile remains a significant drawback. To address this limitation, we have synthesized a homolog of such acids—specifical...
Understanding Li+ solvation structure is critical for the rational design of high- and localized high-concentration electrolytes. Here, we present a systematic investigation of tetrahydrofuran (THF)-based electrolytes with lithium bis(trifluoromethan...
Protein phosphorylation and dephosphorylation reactions of intracellular molecules catalyzed by enzymes such as kinases and phosphatases are essential reactions in a lot of cellular functions such as intracellular signal transduction in living system...
This study aims to investigate the relative stability of the diaminodinitroethylene isomers (cis, trans, and gem). To achieve this goal, calculations at several levels of theory were carried out. The B3LYP, PBE0, and CAM-B3LYP functionals, based on d...
1,3-Dipolar cycloaddition reactions of nitrile imines are a powerful tool for the construction of spirocyclic frameworks, yet controlling chemoselectivity remains challenging when dipolarophiles contain multiple reactive sites. In this study, we inve...
A sustainable hybrid material, CuO/Cu2O, was synthesized using an aqueous extract of Curcuma longa L. as a reducing and stabilizing agent. The material was characterized by UV-Vis spectroscopy, FTIR, XRD, SEM, EDX, and TEM. XRD analysis revealed peak...
Commercially available resorufin was shown to function as an organic photocatalyst for visible-light-induced aqueous radical polymerization under low-irradiance illumination. Polymers with narrow molecular weight distributions and high monomer conver...
The development of a metalloenzyme-like catalytic system for the efficient oxidation of olefins under a dioxygen (O2) atmosphere at room temperature is of significant interest in the field of catalysis. Herein, we present a highly active and selectiv...
In this study, the singlet oxygen photosensitization potential of three natural African plant extracts was investigated using the photooxygenation of α-terpinene (1). Utilizing visible light, the Carpolobia lutea extract achieved high conversio...
A conjugated helical cage, comprising two 1,3,5-tris(phenylethynyl)benzene units connected by diyne linkers, was successfully synthesized. X-ray crystallography revealed helical molecular structures with large twisted angles and a 1:1 mixture of P- a...
Our previous study demonstrated that thiophene-substituted synthetic curcumin analogs possessed better antibacterial activity and stability than natural curcumin, demethoxycurcumin, or bisdemethoxycurcumin in antibacterial photodynamic therapy (aPDT)...
A novel series of Schiff bases (3a–3k), incorporating tranexamic acid (TXA) and phenol-derived aldehydes via imine linkers, was synthesized and structurally characterized. The antimicrobial activity of the compounds was evaluated against a rang...
