An overview on the synthesis and anticancer properties of ethacrynic acid and their analogues

Abstract

Ethacrynic acid (EA, Edecrin) is a well-known diuretic drug used in the treatment of high blood pressure and the swelling caused by diseases such as congestive heart failure, liver failure, and kidney failure. EA has an α,β-unsaturated carbonyl unit which acts as a Michael acceptor involved in the inhibition of the major classes of glutathione S-transferases (GSTs) (α, μ, and π) that plays a crucial role in regulating the multidrug resistance. Moreover, EA was used as an adjuvant to improve the therapeutic efficacy of several anticancer chemotherapeutic agents. EA and their derivatives have received considerable attention in the past decades due to their interesting biological properties. This review highlights the recent development in this area, focusing on their synthesis and their antitumor activities.

Keywords

• Ethacrynic acid
• Diuretic
• Glutathione-S-transferase
• Anti-proliferative activity
• α
• β-unsaturated carbonyl