The　present　study　investigated　the　anticancer　functions　of　ursolic　acid　(UA)　and　its　novel　derivatives,　with　a　nitrogen-containing　heterocyclic　scaffold　and　the　privileged　fragment　at　the　C-28　position　on　apoptosis　induction,　cell　proliferation　and　cell　cycle　in　human　BC　lines.　UA　was　chemically　modified　in　the　present　study　to　increase　its　antitumor　activity　and　bioavailability.　A　novel　UA　derivative,　FZU3010,　was　synthesized　using　a　nitrogen-containing　heterocyclic　scaffold　and　a　privileged　fragment　at　the　C-28　position.　Sulforhodimine　B　assays　were　used　to　measure　the　effect　of　UA　and　different　concentrations　of　FZU3010　on　the　viability　of　breast　cancer　(BC)　SUM149PT　and　HCC1937　cells.　FZU3010　significantly　repressed　the　proliferation　of　the　two　cancer　cell　lines　in　a　dose-dependent　manner,　with　a　half-maximal　inhibitory　concentration　of　4-6　µM,　and　exhibited　decreased　cytotoxicity　compared　with　vehicle-treated　cell　lines.　The　effect　of　FZU3010　on　cell　cycle　distribution　and　cellular　apoptosis　was　also　investigated.　The　results　of　this　investigation　indicated　that　FZU3010　significantly　increased　the　number　of　SUM149PT　and　breast　cancer　HCC1937　cells　in　the　G0/G1　phase　in　a　dose-dependent　manner.　Additionally,　at　a　concentration　of　5　µM,　the　capability　of　FZU3010　to　induce　BC　apoptosis　was　significantly　higher　than　the　capability　of　UA.　Thus,　the　results　of　the　current　study　indicated　that　FZU3010　induced　apoptosis　in　BC　cells,　together　with　induction　of　cell　cycle　arrest　at　the　S　and　G0/G1　phase.　FZU3010　may　therefore　be　considered　as　a　potential　therapeutic　agent　for　the　treatment　of　BC.　©　2018,　Spandidos　Publications.　All　rights　reserved.