Recently　various　drug　candidates　with　excellent　anticancer　potency　have　been　demonstrated,　whereas　their　clinical　application　largely　suffers　from　several　limitations　especially　poor　solubility.　Ursolic　acid　(UA)　as　one　of　ubiquitous　pentacyclic　triterpenes　in　plant　kingdom　exhibited　versatile　antiproliferative　effects　in　various　cancer　cell　lines.　However,　the　unfavorable　pharmaceutical　properties　became　the　main　obstacle　for　its　clinical　development.　With　the　aim　of　development　of　novel　derivatives　with　enhanced　potency,　a　series　of　diversified　UA　amphiphiles　have　been　designed,　synthesized,　and　pharmacologically　evaluated.　Amphiphile　10　(FZU-03,010)　with　significant　improved　antiproliferative　effect　can　self-assemble　into　stable　nanoparticles　in　water,　which　may　serve　as　a　promising　candidate　for　further　development.　©　2016　Elsevier　Ltd