Macrolactins are secondary metabolites mainly from marine microorganisms bearing a unique 24-membered lactone core
structure. Since their first occurrence in 1989, they have attracted considerable attention from natural product chemists, organic chemists,
and pharmacologists due to their chemical complexity, potent antimicrobial and antitumor activities. Some of them are serving as lead
compounds for drug discovery. Although a number of synthetic approaches have been developed, sample supply remains a big issue
which precludes further investigation of pharmacological application and mechanisms of action. This review summarizes current knowledge
about macrolactins including their chemical diversity, biological activities, synthetic studies, and efficient preparation.
Keywords: Antibiotic, antitumor, chemical diversity, efficient preparation, macrolactins, synthesis.
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