Synthesis of a novel CCR1 antagonist for treatment of glioblastoma

Abstract

Glioblastoma is a brain cancer caused by the presence of a fast-growing, malignant tumor in the brain. As of now, this cancer is universally lethal due to lack of efficacious treatment options. C-C chemokine receptor 1 (CCR1) is a G-protein coupled receptor that controls chemotaxis, the movement of cells in response to chemical stimuli. Inhibiting these receptors could retard the growth of the malignant tumor by inhibiting chemotaxis. This research aims to synthesize potential CCR1 antagonists by coupling carboxylic acids with a triazole core. We synthesized these compounds using a simple carboxylic acid coupling and confirmed the identity of the final compounds using nuclear magnetic resonance (NMR) spectroscopy. Further testing of these compounds in inhibition bioassays is planned to be done when lab space becomes accessible again.