Synthesis of Novel Hybrids of Quinazoline and Artemisinin with High Activities against Plasmodium falciparum, Human Cytomegalovirus, and Leukemia Cells.

ABSTRACT: Many quinazoline derivatives have been synthesized over the last few decades with great pharmacological potential, such as antimalarial, anti-inflammatory, antimicrobial, anticancer, and antiviral. But so far, no quinazoline-artemisinin hybrids have been reported in the literature. In the present study, five novel quinazoline-artemisinin hybrids were synthesized and evaluated for their in vitro biological activity against malarial parasites (Plasmodium falciparum 3D7), leukemia cells (CCRF-CEM and CEM/ADR5000), and human cytomegalovirus. Remarkably, hybrid 9 (EC₅₀ = 1.4 nM), the most active antimalarial compound of this study, was not only more potent than artesunic acid (EC₅₀ = 9.7 nM) but at the same time more active than the clinically used drugs dihy

SUBMITTER: Frohlich T 

PROVIDER: S-EPMC6044832 | biostudies-literature | 2017 Jun

REPOSITORIES: biostudies-literature