One-pot three-component synthesis of new triazolopyrimidine derivatives bearing indole moiety as antiproliferative agents

A new series of triazolopyrimidine derivatives was produced via three-component reactions of suitable aromatic orheteroaromatic carboxaldehyde, 3-amino-1,2,4-triazole, and 3-indolyl-3-oxopropanenitrile in triethylamine as a catalyst.The new compounds have been interpreted using elemental analysis, infrared, mass spectrometry, and nuclear magneticresonance spectroscopy. Antiproliferative effects of the new compounds have been screened on four human cancer types andone human noncancerous type (retinal pigment ephitilial-1) via the 3-(4,5-Dimethylthiazol-2-yl)-2,5-DiphenyltetrazoliumBromide assay. Compounds 4a and 4h have moderate activity against the human colon cancer; most of the compoundswere active toward human lung cancer; compounds 4i, 4h, and 4g were highly active on hormone-dependent human breastcancer, while compounds 4c, 4b, 4h, and 4e were the most active on the hormone-independent human breast. The resultsof this study offer a source for further investigation of selected triazolopyrimidine derivatives as antiproliferative agents.

Biopharmaceutical applications of nanogold

The application of nanogold in biopharmaceutical field is reviewed in this work. The properties of nanogold including nanogold surface Plasmon absorption and nanogold surface Plasmon light scattering are illustrated. The physical, chemical, biosynthesis methods of nanogold preparation are presented. Catalytic properties as well as biomedical application are highlighted as one of the most important applications of nanogold. Biosensing, and diagnostic and therapeutic applications of gold nanoparticles are evaluated. Moreover, gold nanoparticles in drugs, biomolecules and proteins' delivery are analyzed. Gold nanoparticles for the site-directed photothermal applications are reviewed as the most fruitful research area in the future

Studies on the anti-inflammatory and analgesic effects of extracts from marine sponges

Two specimens of sponges collected from Red Sea, Egypt, were investigated for their contents of secondary metabolites. The crude extracts of the sponges were tested for their anti-inflammatory and analgesic effects. The toxic effects of the extracts of the two marine sponges were studied. LD50 determination revealed that the investigated extracts of Iregnella and Ircinia sps were 4.69 and 134.7 mg/100g b.wt. respectively, when injected of intraperitoneally in mice. The toxic signs were recorded within the first 24 hrs after injection. Also the two marine sponges extracts showed significant anti-inflammatory and analgesic effects

Synthesis and antimicrobial activity of some 3-[1-phenylethyl]-5-substituted-2H-tetrahydro-1, 3, 5-thiadiazine-2-thione derivatives

In a search for potential antimicrobial compounds thirteen new 3-[1-phenylethyl,]-5- substituted-tetrahydro-2H-1, 3, 5-thiadiazine-2-thiones were synthesized by the reaction of alpha-phenethylamine with carbon disulfide and potassium hydroxide, followed by formaldehyde and the appropriate alkyl, aralkylamines, glycine or ethyl glycinate [Scheme 1]. The chemical structure of the synthesized compounds was elucidated by spectral data and elemental analysis. The title compounds were tested in vitro, for antimicrobial activity against Gram-positive, Gram-negative bacteria, and some fungi, using agar disc method. The antimicrobial activity was found to be affected by the bulkiness of the side chain and presence of polar group at N [5] position. The highest activity was obtained with compounds 41 and 4m [R = CH [2]-COOH, CH [2]- COOC [2] H [5]]

Synthesis and evaluation of the cytotoxic antiviral activities of 5,6-disubstituted isocytosine derivatives

A series of 5,6-disubstituted isocytosines Va, b - XV a, b has been synthesized starting from the key intermediates, 6-methyl- and 6-phenylisocytosines [IIIa, IIIb]. Aminomethylation of these intermediates at C-5 led exclusively to the formation of Mannich bases VIIIa, b - XIIa, b. In addition, a variety of 5-benzoylethenyl derivatives XIIIa, b - XVa, b were synthesized. Depending on the type of secondary amine participating in Mannich reaction, or acetophenone in chalcone formation, different 5,6-disubstituted compounds were prepared in order to study the influence of the substituents on the activity. Moreover, 5-thiocyanato and 5-formyl derivatives were also prepared for evaluation of their biological activity. The cytotoxic activity of some compounds was found to be more potent than the reference st and ard, bropirimine. Preliminary tests for the antiviral activity, using Enterovirus as well as herpes-I virus, indicated stronger activity of some derivatives than bropirimine