Application of Lipophilic Balance Modification in the Creation of Potent Synthetic Anionophores.
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.


METHODS
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.


CONCLUSIONS
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.
Guangdong Provincial Key Laboratory of New Drug Screening, School of Pharmaceutical Sciences, Southern Medical University, Guangzhou 510515. China.
Zhi
Z
Li
Guangdong Provincial Key Laboratory of New Drug Screening, School of Pharmaceutical Sciences, Southern Medical University, Guangzhou 510515. China.
Wen-Hua
WH
Chen
D000838:Anions / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology; D000900:Anti-Bacterial Agents / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D000970:Antineoplastic Agents / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D001424:Bacterial Infections / Q000188:drug therapy*; D006801:Humans; D057927:Hydrophobic and Hydrophilic Interactions; D009369:Neoplasms / Q000188:drug therapy*
D000838:Anions; D000900:Anti-Bacterial Agents; D000970:Antineoplastic Agents
Anion transport activity; anion transporter; channelopathies; ion selectivity; lipophilic balance; lipophilicity