The trans-2,3-disubstituted piperidine, quinazolinone-containing natural product 
febrifugine (also known as dichroine B) and its synthetic analogue, 
halofuginone, possess antimalarial activity. More recently studies have also 
shown that halofuginone acts as an agent capable of reducing fibrosis, an 
indication with clinical relevance for several disease states. This review 
summarizes historical isolation studies and the chemistry performed which 
culminated in the correct structural elucidation of naturally occurring 
febrifugine and its isomer isofebrifugine. It also includes the range of 
febrifugine analogues prepared for antimalarial evaluation, including 
halofuginone. Finally, a section detailing current opinion in the field of 
halofuginone's human biology is included.