ABSTRACT
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.
ABSTRACT
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