New Pyrimidines and Triazolopyrimidines as Antiproliferative and Antioxidants with Cyclooxygenase-1/2 Inhibitory Potential

Abstract

<b>Aim:</b> Cyclooxygenase-2 (COX-2) inhibition and scavenging-free radicals are important targets in cancer treatment. <b>Materials & methods:</b> Sulfanylpyrimidines and triazolopyrimidines were synthesized and evaluated as anticancer and antioxidant COX-1/2 inhibitors. <b>Results:</b> Compound <b>7</b> showed the same growth inhibitory activity as 5-fluorouracil against MCF-7. Compound <b>6f</b> displayed broad-spectrum anticancer activity against the four tested cancer cell lines. Compounds <b>5b, 6a, 6c, 6d</b> and <b>8</b> were found to be more active antioxidants than trolox. Compounds <b>6a, 6c, 6f</b> and <b>8</b> revealed high COX-2 inhibitory activity and selectivity, which was confirmed by docking studies. <b>Conclusion:</b> Compound <b>6f</b> could be considered as promising anticancer and antioxidant structural lead with COX-2 inhibition that deserve further derivatization and investigation.