From Sea Sponge to Clinical Trials: Starting the Journey of the Novel Compound PM742

Abstract

PM742 (1), a new chemical entity, has been isolated from the sponge Discodermia du Bocage collected in the Pacific Ocean. This compound showed strong in vitro cytotoxicity against several human tumor cell lines as well as a tubulin depolymerization mechanism of action, which led us to conduct an extensive Structure-Activity-Relationship study through the synthesis of different analogs. As a result, a derivatively named PM534 (2) is currently in its first human Phase I clinical trial. Herein, we present a comprehensive review of the isolation, structural elucidation, and antitumor activities of the parent compound PM742.

Keywords

• sponge
• <i>Discodermia du Bocage</i>
• cytotoxicity
• isolation
• structural elucidation
• tubulin interaction