The Effect of Polysubstituted Pyrrole Compounds on the Inflammatory Response

Polysubstituted pyrrole compounds, developed by Dr. John Gupton in the chemistry department at the University of Richmond, have shown success as chemotherapeutic agents. The pyrrole moiety targets microtubules, an essential component of the cell’s cytoskeleton and active participant in mitosis (Fig. 1). Colchicine, an antimitotic agent that has been used to treat a number of ailments ranging from gout to back pain, acts as a microtubule depolymerizer. Since its discovery, the site to which it binds on tubulin has been commonly referred to as the ‘colchicine site.’ Pyrroles bind to the ‘colchicine site’ and also behave as potent microtubule depolymerizers, causing a loss of cellular microtubules, hindrance of mitotic spindle function, mitotic arrest, and apoptosis initiation.1 This activity, specifically, is why microtubule targeting drugs are becoming instrumental in the development of cancer treatment