Objective: Synthetic anionophores are created to mediate the transmembrane transport of
anions across phospholipid bilayer membranes. By replacing the defective natural anion channels, they
are thought to have high potentials as chemotherapeutic agents for the treatment of channelopathies.
Method: In addition, there is a hope that synthetic anionophores may serve as therapeutic agents for
cancers and bacterial infections. Because of the amphiphilicity of phospholipid bilayer membranes,
lipophilicity has been well studied as one of the most important structural factors that affect the activity
of synthetic anionophores. This paper reviews the application of lipophilic balance modification in the
creation of effective synthetic anionophores during the past few years.
Conclusion: The strategies that have been widely used to change the lipophilicity are introduced. In
addition, the important role of optimal lipophilicity in terms of logP in the rational design of synthetic
anionophores is also discussed.