Mohamed, A. A. RadwanFahad, M. AlminderejHala, E. M. TolanHanem, M. Awad2020-10-162020-10-162020-09Mohamed A. A. Radwan, Fahad M. Alminderej, Hala E. M. Tolan, Hanem M. Awad. One-pot three-component synthesis of new triazolopyrimidine derivatives bearing indole moiety as antiproliferative agents. Journal of Applied Pharmaceutical Science. 2020 Sep; 2020 Sep: 012-0222231-3354http://imsear.searo.who.int/handle/123456789/210658A 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.Triazolepyrimidineindolemulticomponent reactionantiproliferative.Journal ArticleIndiaDepartment of Chemistry, College of Science, Qassim University, Buraydah, Kingdom of Saudi Arabia.Applied Organic Chemistry Department, National Research Center, Dokki, 12622, Egypt.Department of Chemistry, College of Science, Qassim University, Buraydah, Kingdom of Saudi Arabia.Department of Photochemistry, National Research Centre, Dokki, 12622, Cairo, Egypt.Tanning Materials and Leather Technology Department, National Research Centre, Dokki, Cairo, 12311, Egypt