Currently,　there　is　a　renewed　interest　in　common　dietaries　and　plant-based　traditional　medicines　for　the　prevention　and　treatment　of　cancer.　In　the　search　for　potential　anticancer　agents　from　natural　sources,　ursolic　acid　(UA),　a　pentacyclic　triterpenoid　widely　found　in　various　medicinal　herbs　and　fruits,　exhibits　powerful　biological　effects　including　its　attractive　anticancer　activity　against　various　types　of　cancer　cells.　However,　the　limited　solubility,　rapid　metabolism　and　poor　bioavailability　of　UA　restricted　its　further　clinical　applications.　In　the　past　decade,　with　substantial　progress　toward　the　development　of　new　chemical　entities　for　the　treatment　of　cancer,　numerous　UA　derivatives　have　been　designed　and　prepared　to　overcome　its　disadvantages.　Despite　extensive　effort,　discovery　of　effective　UA　derivatives　has　so　far　met　with　only　limited　success.　This　review　summarizes　the　current　status　of　the　structural　diversity　and　evolution　in　medicinal　chemistry　of　UA　analogues　and　provides　a　detailed　discussion　of　future　direction　for　further　research　in　the　chemical　modifications　of　UA.　©　2015　Elsevier　Masson　SAS.