Abstract

ABSTRACT
A new series of triazolopyrimidine derivatives was synthesized by a one-pot three-component reaction of suitable aromatic or heteroaromatic carboxaldehyde, 3-amino-1,2,4-triazole, and 3-indolyl-3-oxopropanenitrile in TEA as a catalyst. The structures of the new compounds have been confirmed by elemental analysis, IR, NMR and, mass spectroscopy. Antiproliferative effects of the newly synthesized compounds have been screened on four human cancer types and one human non-cancerous type (RPE-1) via the MTT assay. Compounds 4a and 4h have a moderate activity against the human colon cancer; most of the compounds were active towards human lung cancer; compounds 4i, 4h, and 4g were highly active on hormone-dependent human breast cancer, while compounds 4c, 4b, 4h, and 4e were the most active on the hormone-independent human breast. The results of the study offer a source for further investigation of selected triazolopyrimidine derivatives as antiproliferative agents.

Key words: triazole; pyrimidine; indole; multicomponent reaction; antiproliferative.