We have achieved the total synthesis of an architecturally and biologically intriguing cyclic polypeptide,rhizonin A(1),in an exceptionally concise and convergent fashion.The strategic route entails 9 longest linear steps to elaborate commercially available materials into the natural product with an overall yield of 9.7％.The brevity of sequence and high overall yield was fueled by the judicious selection of chemical tactics.Rhizonin A(1)showed weak inhibitory effects on the cell viability of HCT116 colorectal cancer cells and this activity was dependent on hypoxia-inducible factors.