Recent developments in phosphorus-containing ester prodrugs and its prospectives

Prodrugs has been established as a strategy to improve the medical properties of their parent drugs, and thereby enhance the possibility of these potential drugs to cure the disease but this modified drugs should be cautious as their properties like issue distribution, efficacy and toxicity may change. In the current developed modifying strategies, esterification is among the most common ones, which masks charged hydrophilic groups with ester promoieties so that permeation ability of drugs through the membrane will enhance. Among various esters, phosphorus-containing ester prodrugs are attractive due to close relationship between atom phosphorus and key bioactive compounds including DNA or RNA, phospholipid, proteins. Herein, we will review the developments of these prodrugs, especially phosphate and phosphonate prodrugs, their synthetic methods, pros and cons, application and methods for characterization, with which specific examples or clinical trials will be attached for clearer description Ultimately, we prospect that the phosphorus-containing prodrugs will for certain be further studied and improved and be an indispensable role in medical cares.