Suppressive potencies of tetrandrine, isotetrandrine, fangchinoline, berbamine, dauricine, cepharanthine, and armepavine on expression and activation of NF-κB in MOLT-4 cells, MOLT-4/DNR cells, peripheral blood mononuclear cells (PBMCs) of healthy subjects and PBMCs of dialysis patients were compared. In MOLT-4 cells, the suppressive potencies evaluated by the IC50 values were isotetrandrine > cep

A series of triphenylphosphonium (TPP) conjugates of 1,2,3-triazolyl analogues of several pyrimidine nucleosides was synthesized and evaluated for the in vitro cytotoxicity against human cancer cell lines M-HeLa, MCF-7, PANC-1, PC-3, DU145, SKOV-3, A275, and normal human cell line WI-38. In these TPP-conjugates triphenylphosphonium cation was attached via a tetramethylene chain to the N-3 atom of the

A series of long-chain imidazolium-based ionic liquids (ILs) 1-dodecyl-3-methylimidazolium chloride (1), 1,3-bis(octyloxycarbonylmethyl)imidazolium chloride (2) and 1-dodecyloxycarbonylmethyl-3-methyloxycarbonylmethylimidazolium chloride (3), were synthesized and evaluated as antimicrobials against a wide range of bacteria and fungi. Toxicological risks of selected compounds were assessed using the

In the present study, a novel series of quinazoline derivatives is developed for cancer therapy. All the synthesised analogues were evaluated against a panel of 60 human cancer cell lines for the antiproliferative activity. Significant and selective growth inhibition of several solid tumour cell lines such as NCI-H322M, NCI-H522 (non-small cell lung cancer), IGROV1, SK-OV-3 (ovarian cancer), TK-10

Cola belongs to the family Malvaceae and contains 125 Cola plants. Among the Cola species, Cola acuminata and Cola nitida are the most studied for their pharmacology effects. Cola contains phytochemicals such as alkaloids, caffeine, theobromine, theophylline, quinic acid, chlorogenic acid, purine, (−)-epicatechin, (+)-catechin, sterols, anthraquinones, flavonoid glycosides, cardenolides, tannins, rostratanic

A multicomponent reaction was used as a synthetic strategy to prepare organotin (IV) complexes, 2-amino-3-hydroxypyridine, saliciladehydes 5-R-substituted (H, CH3, OCH3, C(CH)3, F, Cl, Br, I, NO2), and dibutyltin(IV) oxide were used as starting materials. The complexes were analyzed by IR, UV–Visible, MS, NMR of 1H, 13C, 119Sn. The complex 3a was structurally identified by X-ray crystallography, which

The Yamaguchi reaction is widely and generally applied to synthesize esters and lactones. It involves 2,4,6-trichlorobenzoyl chloride as the Yamaguchi reagent, 4-dimethylaminopyridine, and triethylamine. Pyrazinamide is a crucial first-line drug for tuberculosis treatment, therefore their analogues are interesting in organic synthesis. In general, the synthesis pyrazinamide analogues involve reaction

Two aryl-enclosed polyketides were identified from the ethyl acetate extract of mangrove sediment associated bacterium Bacillus amyloliquefaciens, and were characterized as 1-(8-hydroxy-1-oxoisochroman-3-yl)propyl 4′-(6′-hydroxy-8′-oxotetrahydrofuran-5′-yl)acetate (compound 1) and 6′a-(3′-(1′-(8-hydroxy-1-oxoisochroman-3-yl)propoxy)-3′-oxoethyl)-8′-oxotetrahydrofuran-6′-yl butyrate (compound 2) by

Many chemicals found in mangroves reportedly exhibit potent anticancer, antibacterial, anti-inflammatory, antioxidant, and antitumor properties. Several of such compounds include feature unique structures and display interesting pharmacological effects. Few medicinal mangrove plants from Vietnam have been characterized with regard to their chemical constituents. Aegiceras corniculatum (L.) Blanco is

Enhancer of zeste homolog 2 (EZH2) is responsible for the methylation of lysine 27 of histone H3 (H3K27) leading to transcriptional repression. Consequently, EZH2 is related with several diseases including cancers, as overexpressed EZH2 can down-regulate cancer suppressor genes. Therefore, EZH2 became a promising target for cancer treatment and diagnosis and in vivo imaging of EZH2 is critical for

Cervical cancer (CC) is the most common gynecological cancer and is one of the results of high-risk HPV infection. Recent statistics demonstrate that 90% of cervical cancer cases are diagnosed in low- and middle-income countries. These results are observed due to the poor sanitation and lack of proper preventive strategies. Quercetin is a plant compound with a great number of beneficial properties

A disease emerged in the city of Wuhan, Hubei Province, Central China in the last month of 2019. It was pneumonia caused by a newly emerged coronavirus called COVID-19, later. Coronaviruses are enveloped RNA viruses belong to the Betacoronavirus family and infected birds, humans, and other mammals. In March 2020, the World Health Organization declared the COVID-19 outbreak could be characterized as

Two undescribed polyoxygenated furanocembranoid derivatives, methyl 15-(9-hydroxy-8-methoxy-2,12-dimethyl-15-oxa-bicyclo[10.2.1]pentadeca-2,4,6,11-tetraen-3-yl)propanoate (salmacembrane A) and 1-(16-methyl-2,16-dihydrofuran)-8-methoxy-12-methyl-20-oxabicyclo[10.2.1]pentadeca-2,4,6,11-tetraen-9-ol (salmacembrane B), were isolated from the organic extract of sea urchin Salmacis bicolor (family Temnopleuridae)

The 3-hydroxy-N-(p-hydroxy-phenethyl) phthalimide (HNHP), which showed in vitro peroxisome proliferator-activated receptor-γ (PPAR-γ) activation and in vivo anti-inflammatory effect in our previous study, was speculated to be a dual-target lead compound because similar structures exhibited α-glucosidase inhibitory activities. To investigate the dual targeting potential, molecular docking of HNHP was

Leishmaniasis is a much-neglected tropical disease, especially in developing countries. Visceral Leishmaniasis (VL) is the most severe form of this infection caused by Leishmania infantum specie. It affects the splenic and hepatic systems and, when left untreated, it is fatal in 95% of cases. There is no human vaccine available and the recommended treatment not only presents adverse effects but it

This study is aimed at extracting and purifying bioactive peptides from white grub larvae (Polyphylla adspersa) hydrolysate and examining their antioxidant effects on lung cancer cells (A549). Bioactive peptides from white grub larvae hydrolysate (WGLH) were produced using papain, pancreatin, proteinase-K and trypsin. The results showed that papain hydrolysate had the most 1, 1-diphenyl-2-pycryl-hydrazyl

In this study, 15 new 1H-benzimidazole-5-carboxamidine derivative compounds that could be new antimicrobial agents were synthesized and their antimicrobial activities were determined using the microdilution method. When the activity results were examined, it was observed that the antibacterial effects of the new benzimidazole derivatives were weaker than standard drugs, but some derivatives showed

Natural and synthetic naphthoquinones have demonstrated numerous biological activities; therefore, they provide an interesting scaffold for medicinal chemists in the search for new drugs. A series of amino alcohol derivatives from 1,4-naphthoquinone with a free (2a–e) and acetylated (3a–d) hydroxyl group were synthesized, characterized, and evaluated as antioxidant agents employing 1,1-diphenyl-2-picrylhydrazyl

A novel series of 1-(5-(benzylthio)-1,3,4-thiadiazol-2-yl)-3-phenylurea derivatives (5a–l) were designed and synthesized as sorafenib analogs. The in vitro cytotoxicity effects of synthesized compounds were evaluated against four different human cancer cells including MCF-7, HepG2, A549, and HeLa cell lines. The biological results showed that most of the compounds significantly prevented the proliferation

Macrocyclic compounds of multifaceted structural scaffolds are being increasingly reported from the marine environment, and gaining commercial importance due to their ability to inhibit the pro-inflammatory mediators. An unreported polyether macrocyclic polyketide characterized as 6-(butoxy)-13,15,22-trihydroxy-3,18-dioxatricyclo[18.3.1.011,16]tricosa-9,20-diene-4,8-dione was isolated from the marine

Alzheimer’s disease (AD) is the most common form of dementia that affects more than 40 million people around the world. The incidence is expected to rapidly increase due to the lack of any effective treatment. In previous work we synthesized a family of five ionophoric polyphenols (compounds 1–5) that targeted important aspects related to AD, such as the toxic aggregation of amyloid-β peptides, the

Series of novel analogs, which were primarily modified on its lactone moiety, was synthesized based on Andrographolide (1), a natural product sesquiterpene inhibitor of α-glucosidase. Among new analogs, 14-deoxy-11,12-didehydro-15-(4-ethoxybenzylidene)andrographolide (3h) was determined to have the greatest potential of α-glucosidase inhibitor through the calculation of IC50 value of 160 ± 5.1 μM,

In the current experimental study, we have synthesised new monocarbonyl curcumin analogues bearing propargyl ether moiety in their structure and evaluated for in vitro antifungal and radical scavenging activity. The antifungal activity was carried out against five human pathogenic fungal strains such as Candida albicans, Fusarium oxysporum, Aspergillus flavus, Aspergillus niger and Cryptococcus neoformans

Malaria, a nocuous disease, which has become a major challenge for the health resulting in deaths of millions of people around the globe. Malaria is a parasitic disease propagated by mosquitoes and infects the human beings. Several species of Plasmodium are responsible for this life-threatening disease and Plasmodium falciparum being the most virulent. In order to eradicate the malarial parasite, the

The second-generation XPhos palladium preformed catalyst-based C–N cross-coupling through Buchwald–Hartwig amination with primary and secondary amines towards functionalized benzoxazepino(7,6-b)quinolines is accounted for. The microwave irradiation in dioxane provided the desired highly functionalized oxazepino quinolines, 5, in high yield and purity from the corresponding 2-chloro-3-formyl quinolines

The [1,2,4]triazolo[1,5-a]pyrimidines (TPs) comprise an important class of non-naturally occurring small molecules that aroused the interest of researches. This scaffold is present in diverse important structures in agriculture and medicinal chemistry, such as antibacterial, antifungal, antiviral, antiparasitic, and anticancer. As over the decades the development of the chemistry and application of

The study investigated the anti-urease and cytotoxic activities of two major essential oil compounds; 1-Nitro-2-phenylehtane (NPE) and Nerolidol, isolated from the acetone extract of Dennettia tripetala (Pepper Fruit) seeds. Structural characterization of these compounds was performed by NMR, E1MS, and FT-IR spectroscopic techniques. Anti-urease activity of the compounds on Jack bean Urease was accessed

A novel series of N-methyl/benzyl-substituted benzimidazolyl-linked para-substituted benzyl-based compounds containing 2,4-thiazolidinediones, dimethyl malonate (DMM), and diethyl malonate (DEM) 17–27 were designed, docked, synthesized, and evaluated for their antidiabetic activity studies. Structures of all the synthesized compounds were confirmed through 1H NMR, 13C NMR, FTIR, and mass spectrometry

The water-soluble sulfated derivatives, apigenin-8-sulfonate sodium (AS) and apigenin-3′, 8-disulfonate sodium (ADS) derived from parent apigenin (AP), were synthesized and characterized by infrared (IR) spectra, hydrogen nuclear magnetic resonance (1H NMR), carbon nuclear magnetic resonance (13C NMR), high-resolution mass spectra (HRMS), and elemental analysis. The mice model of hepatotoxicity induced

Coronavirus disease (COVID-19) pandemic is caused by severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2). COVID-19 is a global health emergency and no clinically approved vaccines or antiviral drugs available to date. Intensive research on SARS-CoV-2 is urgently warranted to understand its pathogenesis and virulence mechanisms and to discover target-based antiviral therapeutics. Among various

α-Glucosidase plays a major role in degradation of carbohydrates to glucose. Therefore, inhibition of this enzyme can be useful in the treatment of carbohydrate-related diseases such as diabetes, cancer, and viral infections. In this study, a new series of acridine-9-carboxamide linked to 1,2,3-triazole-N-phenylacetamide derivatives 5a–m were designed, synthesized, and evaluated as potent α-glucosidase

Saponins are a class of amphipathic glycosides prevalent in various plant species. They are very important for human health and may be used in various drug formulations. Saponins play vital roles in inhibition of many singling pathways such as PI3K/AKT pathway, AKT/MAPK pathway, EGFR/PI3K/AKT pathway, PI3K/AKT/mTOR pathway, and RNF6/AKT/mTOR pathway. They have been reported to exhibit cytotoxic activities

A new series of naphthyl chalcones (3a–3p) and their pyrazoline derivatives (4a–4h) were synthesized using substituted acetophenones, substituted naphthaldehydes, and hydrazine hydrate as starting materials. All the synthesized compounds were characterized by IR, NMR, and mass spectrometric analysis and screened for antimycobacterial activity against Mycobacterium tuberculosis H37Rv (ATCC 27924) and

Novel unsaturated piperazine and homopiperazine derivatives (3a–h) were synthesized in medium to good yields by acylation reactions of piperazine and homopiperazine with methacrylic anhydride (2a) and benzoyl chloride (2b). Piperazine containing dihydrofuran compounds (5a–l) were obtained from radical addition and cyclizations of 3a–h with 1,3-dicarbonyl compounds such as dimedone (4a), ethyl acetoacetate

In this study, we synthesize 2-amino-4-alkyl/aryl-6-(hydroxymethyl)-8-oxopyrano[3,2-b] pyran-3-carbonitriles derivatives using a multicomponent reaction featuring aromatic or aliphatic aldehydes, kojic acid, and malononitrile catalyzed by nano fluoroapatite doped with Si and Mg (Si–Mg–FA). All reactions were carried out in EtOH as the solvent under reflux and green condition. The process demonstrates

A series of some novel (E)-2-methyl/propyl-4-[(2-(substitutedbenzylidene)hydrazinyl]-5,6,7,8-tetrahydrobenzo[4,5]thieno[2,3-d]pyrimidines was synthesized and characterized by adopting an appropriate synthetic scheme. The effect of electron withdrawing and electron donating groups at the aromatic ring in presence of methyl and propyl substituents at the 2-position of the scaffold was evaluated for anthelmintic

In this work we report the structure–affinity relationships, binding properties, and metabolic stability studies of a series of benzo[d]thiazol-2(3H)one as sigma receptor (σR) ligands. Specifically, to improve the metabolic stability of the cyclic amine fragment of our lead compound (SN56), the metabolically unstable azepane ring was replaced with a 1-adatamantamine moiety. Within the synthesized analogs

Pseudotrachydium kotschyi is a native medicinal plant used as a local medicine from Lorestan province of western Iran having numerous biological properties. After GC−MS analysis of Pseudotrachydium kotschyi essential oils (PKEOs), some biological activities were investigated. Additionally, TNF-α and TGF-β1 were studied in Leishmania-infected macrophages (in vitro) and Carrageenan-induced paw edema

The synthesis and screening of several fusaric acid (FA) and analogues against five common clinical pathogens (gram-positive and gram-negative) and in vitro hemolytic activity assay in human red blood cells, for the first time, were reported. The biological results reveal that FA and its analogues exhibited moderate antimicrobial activities. Compounds 2–5 and 7 showed growth inhibitory activity in

Epilepsy is one of the most common neurological disorders worldwide and it requires a long-term or life-long treatment. Current standard treatment includes the use of antiepileptic drugs. To date, many organic compounds have been synthesized by chemists as potential antiepileptic drugs and their anticonvulsant properties have been investigated. While evaluating the anticonvulsant activities of these

A series of derivatives of 5-hydroxyalkylamino-1,3-oxazoles were synthesized. Among these derivatives, 5 compounds have been evaluated for their activities against a normal laboratory human cytomegalovirus (HCMV) strain, AD169, in human foreskin fibroblast (HFF) cells. Bioassays showed that among these, 2 compounds containing a remainder of glucamine exhibited moderate antiviral activity (compounds

Bioisosteric replacements are often tried goaling to affect the lipophilicity, polarity, and aqueous solubility of the substances, as a way to obtain therapeutically improved medicines. Also, hydrazonyl compounds are described with a wide range of pharmacological activities, having also recognized activities in antimycobacterial field. In this study, twenty-seven pyrimidinyl and pyrazinyl derivatives

A novel library of chalcone linked thiazole-imidazopyridine (12a–j) derivatives were designed, synthesized, and their structures were characterized by 1H NMR, 13C NMR and mass spectral studies. Further, all compounds were tested for their anticancer effects on four human cancer cell lines including MCF-7 (breast carcinoma), A549 (lung carcinoma), DU-145 (prostate carcinoma) and MDA MB-231 (breast carcinoma)

Three esters of rhodamine B (1–3) differing in their alkyl chain lengths as well as several rhodamine B amides (4–9) were synthesized in good yields and tested for their cytotoxicity in SRB assays employing several human tumor cell lines. The rhodamine B esters were unselective but showed cytotoxicity of as low as EC50 = 0.15 ± 0.02 µM. The rhodamine B amides were slightly less cytotoxic but showed

Cancer is often associated with chronic inflammation. In order to develop potential anticancer and anti-inflammatory agents a series of 26 diarylidenecyclopentanones (DACPs) Ia–Iv, II, III, and IV were synthesized. Five of the synthesized DACPs are novel (Ih, Ij, Ik, Is, and Iv), derivative Iv was characterized using single-crystal X-ray diffraction study. All the synthesized derivatives were tested

N-alkylated and O-alkylated anthraquinone derivatives with structures analogous to mitoxantrone were synthesized, characterized, and evaluated for their cytotoxic properties against three tumor cell lines (Human Breast Adenocarcinoma MCF-7, Human Cervical Adenocarcinoma HeLa, and Human Glioblastoma M059J) and a normal cell line (human lung fibroblasts GM-07492A). A structure-activity relationship study

Leishmaniasis is a severe disease caused by protozoa of the genus Leishmania. The disease affects millions of people. Treatment is limited to only a few drugs that cause severe side effects. The identification of new compounds to treat leishmaniasis remains a challenge. This study aimed to determine the chemical composition of Eugenia moraviana fruit extract (EmCE) and to investigate its effect on

A library of indolinedione–coumarin hybrid molecules was rationally designed and synthesized against hyperuricemia. All of the synthesized hybrid molecules were tested to check their inhibitory activity against xanthine oxidase enzyme by using a spectrophotometric assay. The results revealed that the compound showed IC50 values within the range of 6.5–24.5 µM amongst which compound K-7 was found to

To continue the research on the preparation of resveratrol structural analogs containing the 3-pyridinol fragment, a series of derivatives with an ethyl radical sterically shielding the hydroxyl group was synthesized. It was shown that the ethyl group introduction has an ambiguous effect on the radical scavenging and antioxidant properties of the stilbazoles studied, which is probably related to the

We are aiming in this work to synthesize target molecules not only possess antitumor activities but also kinase inhibitors. The target molecules were obtained from dimedone, which reacted with triethoxymethane to produce a product that is capable for many heterocyclization reactions to give fused pyrazole, thiophene and isoxazole derivatives. Compounds 7b, 7c, 7d, 9b, 11, 12c, 12d, 14b, 16b, 17c, 17d

The aberrant protein–protein interaction between calmodulin and mutant huntingtin protein in Huntington’s disease patients has been found to contribute to Huntington’s disease progression. A high-throughput screen for small molecules capable of disrupting this interaction revealed a sultam series as potent small-molecule disruptors. Diversification of the sultam scaffold afforded a set of 24 analogs

The most common mechanism of the resistance to β-lactam antibiotics is the expIdentification of cisplatin and palladiuression of β-lactamases, which can hydrolyze the β-lactam moiety and deactivate these antimicrobials. The worldwide prevalence of New Delhi metallo-β-lactamase-1 (NDM-1), also known as carbapenemase has created distress among clinicians. NDM-1 is a type of metallo β-lactamase (type

A series of (E)-1,2-diarylethylidenehydrazine carboximidamides 2a–j were synthesized and characterized by NOESY experiment as anticonvulsant agents and their antiseizure activity was evaluated by intracerebroventricular administration of compounds. Most of the compounds had significant protection against tonic-clonic seizures and 2a was found to be as equipotent as carbamazepine in seizures control