ObjectiveIn an effort to etablish new candidates with improved antineoplastic activity, 4-cycloalkylidineamino 1,2-naphthoquinone semicarbazones were synthesized, characterized and evaluated for anticancer activity.
A series of N-nitroso-2,6-diarylpiperidin-4-one semicarbazones and thiosemicarbazones were synthesized, characterized by IR, NMR and elemental analysis. All the compounds were screened for their antibacterial activity against Gram-positive bacteria Bacillus subtilis, Staphylococcus aureus and Gr...
In the present study we have designed a new pharmacophore ‘Chalconesemicarbazone’ by pharmacophore hybridization approach of drug design. A series of novel chalconesemicarbazones was synthesized and evaluated for their antioxidant activity by reducing power assay. Most of the compounds were fo...
A number of N-(4,6-substituted diphenylpyrimidin-2-yl) semicarbazones (4a–t) were synthesized and tested for their anticonvulsant activity against the two seizure models, maximal electroshock seizure (MES) and subcutaneous pentylenetetrazole (scPTZ). All the synthesized compounds possessed the ...
Acid-catalyzed cyclization of 4-(γ-oxoalkyl)semicarbazide hydrazones has been studied. 7-Membered cyclic semicarbazones, 2,4,5,6-tetrahydro-3H-1,2,4-triazepin-3-ones, were obtained from the γ-phenyl-substituted semicarbazides, while the cyclization of the γ-methyl-substituted semicarbazides i...
Stereoselectivity of acid-catalyzed cyclization of 4-(1-aryl-3-oxobutyl)semicarbazide hydrazones into mixtures of trans- and cis-isomers of 14-membered cyclic bis-semicarbazones has been studied. The isomer ratio is dependent on solvent, catalyst acidity, substrate structure and concentration, r...
Urease is a bacterial enzyme that is responsible for virulence of various pathogenic bacteria such as Staphylococcus aureus, Proteus mirabilis, Klebsiella pneumoniae, Ureaplasma urealyticum, Helicobacter pylori and Mycobacterium tuberculosis. Increased urease activity aids in survival and coloni...
A series of carbonate-containing antacids was examined by IR and X-ray analysis to establish the role of carbonate and to compare the structure of the antacids to naturally occurring carbonate minerals. Based on IR analysis, the relative degree of perturbation of carbonate increases in the order...
Approximately 90% of the sodium present in a washed aluminum hydroxycarbonate gel was removed by exchange with magnesium. This behavior supports recent structural studies which have suggested that cations such as sodium serve as counterions in aluminum hydroxycarbonate gel. However, sodium could...
The antiulcer effect of DASC has previously been described by the authors using histamine-induced ulceration of guinea pigs as the criterion. These phenomenaare believed to be due to the increased gastric acid secretion produced by the histamine, therefore, the mechanism of the antiulcer activit...
The methanol and water solvents were used for the production of hydrogen from potassium borohydride. In addition, phosphoric acid was selected as the green catalyst so that this semi-methanolysis reaction would be more effective for the first time. The semi-methanolysis of potassium borohydride ...
A novel method for the rapid dissolution of fused silicates in mineral acid is described. Fusion with 2.5 g of a KBO2-K2CO3 (3:2, w/w) mixture in a platinum crucible at 1000 °C will decompose 0.1 g of silicate samples such as basalt rock, glass sand and powdered glass in 10 min, and the cooled ...
Strontium metaborate (SrB2O4) is a suitable material for use as a matrix for luminescent dopant ions. Similarity of ionic radii of strontium and divalent europium makes it an excellent host for Eu dopant. This paper reports on the Czochralski growth and spectroscopic study of SrB2O4 single cryst...
Podophyllin, an ethanolic extract of Podophyllum peltatum L. or P. emodi Wall (syn. P. hexandnum Royle), is a good source of the aryltetralin-type lignan, podophyllotoxin. The latter compound, as well as its congeners and derivatives exhibit pronounced biological activity mainly as strong antivi...
Podophyllotoxin is currently in high demand as the lead chemical precursor for the anti-cancer drugs etoposide and teniposide. We conducted a two-phase study: (i) screening of Juniperus and other related species and identified Juniperus virginiana as the species with the highest podophyllotoxin ...
ABSTRACTThe aryltetralin-type lignan podophyllotoxin, the main agent present in the resin extracted from the rhizomes of different podophyllum species, possesses important antineoplastic and antiviral properties and has been widely used in diverse cultures since ancient times for medicinal purpo...
A series of perbutyrylated glycosides of podophyllotoxin and its derivatives were synthesized and evaluated for their antitumor activity in vitro. Most of them exhibit cytotoxic activity against a panel of five human cancer cell lines (HL-60, SMMC-7721, A-549, MCF-7, SW480) using MTT assays. Amo...
Three series of novel sulfonylurea podophyllotoxin derivatives were designed, synthesized, and evaluated for in vitro cytotoxicity against four tumor cell lines (A-549, DU-145, KB and KBvin). Compounds 14c (IC50: 1.41–1.76 μM) and 14e (IC50: 1.72–2.01 μM) showed superior cytotoxic activity c...
Pulsed electric field technology (PEF) was applied to Podophyllum peltatum as a novel approach to enhance the extraction of podophyllotoxin. Podophyllotoxin is a valuable for the treatment of cancer and venereal warts. However, the demand for podophyllotoxin exceeds the supply and conventional e...
The present study was conceptualized with the aim of developing a safe radioprotector for human application against radiation induced toxicity. For this study, a formulation (G-002M) prepared by combining three active principles isolated from rhizomes of Podophyllum hexandrum, was evaluated for ...
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