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Recently, it has become obvious that renin-angiotensin system (RAS) plays an important role in cancer progression through angiotensin converting enzyme (ACE), involving activation and upregulation of multiple oncogenic molecules. Accordingly, suppression of ACE and its subsequent downstream cascades has received considerable attention as a possible way to combat oncological diseases. In this book chapter, the role of a several plant-derived phenolic acids (Ellagic acid, Gallic acid, Caffeic acid) on inhibition of ACE is demonstrated, and involvement of this action in chemopreventive and chemotherapeutic properties of these natural compounds is discussed, with a special focus on antiangiogenic and antiinflammatory activities.