Kristina Pavić, Goran Poje, Lais Pessanha de Carvalho, Tana Tandarić, Marina Marinović, Diana Fontinha, Jana Held, Miguel Prudêncio, Ivo Piantanida, Robert Vianello, Ivona Krošl Knežević, Ivana Perković, Zrinka Rajić
Although cancer and malaria are not etiologically nor pathophysiologically connected, due to their similarities successful repurposing of antimalarial drugs for cancer and vice-versa is known and used in clinical settings and drug research and discovery. With the growing resistance of cancer cells and Plasmodium to the known drugs, there is an urgent need to discover new chemotypes and enrich anticancer and antimalarial drug portfolios. In this paper, we present the design and synthesis of harmiprims, hybrids composed of harmine, an alkaloid of the β-carboline type bearing anticancer and antiplasmodial activities, and primaquine, 8-aminoquinoline antimalarial drug with low antiproliferative activity, covalently bound via triazole or urea...
April 23, 2024: Bioorganic & Medicinal Chemistry