Triple-negative　breast　cancer　(TNBC)　has　a　poorer　prognosis　than　other　subtypes　of　breast　cancer;　however,　it　lacks　effective　targeted　therapies　clinically.　In　this　study,　we　found　FZU-0038-056,　a　novel　compound　derived　from　last-stage　functionalization　of　tetrahydro-beta-carboline　scaffold,　showed　the　most　potent　anti-cancer　activity　against　TNBC　cells　among　the　42　synthesized　derivatives.　We　found　FZU-0038-056　significantly　induces　apoptosis　in　HCC1806　and　HCC1937　TNBC　cells.　FZU-0038-056　reduces　the　expression　levels　of　several　anti-apoptosis　proteins,　including　Bcl-2,　Mcl-1　and　XIAP.　Furthermore,　we　found　FZU-0038-056　induces　apoptosis　partially　through　inhibiting　the　expression　of　Bcl-2.　Finally,　we　found　FZU-0038-056　significantly　suppresses　HCC1806　xenograft　tumor　growth　in　nude　mice　without　affecting　their　body　weight.　Therefore,　FZU-0038-056　has　the　potential　to　be　a　new　anticancer　agent　for　treating　human　TNBC.