Diarylpentanoids with antitumor activity: A critical review of structure-activity relationship studies

Abstract

Diarypentanoids are commonly considered as monocarbonyl analogues of curcumin. Since the discovery of this compound in 1962, twenty one diarylpentanoids have been isolated and almost 600 synthetic analogues with antitumor activity have been synthesized. This review reports the exploitation of diarylpentanoids to develop curcumin analogues with improved antitumor activity over the last two decades. The mechanism of action and structure-activity relationship (SAR) studies are also highlighted. More importantly, structural features for the antitumor activity that may guide the design of new and more effective diarylpentanoids are also proposed.

Keywords: Antitumor activity; C5-curcuminoids; Chemotherapy; Curcumin; Diarylpentanoids; Structure-activity relationship.