In this thesis, the solution phase synthesis scheme and the classic ″3+2″ synthesis scheme was employed. Also the route was started from D-Phenyline and D -Leucine as raw materials. The linear peptapeptide was synthesized by protecting and deprotecting the amine, deprotecting the acid, methylating the amino acid, coupling and other steps. The cyclization step was completed by mixed condensation reagents with DEPBT, HATU and TBTU. Herein, two Galaxamide analogues HW-1 and HW-2 were synthesized, characterized by 1H-NMR, 13C-NMR, ESI-MS and ICP-MS. The in vitro anticancer activities of the target compounds were evaluated through MTT assays against various human cancer cell lines. It shows that they both exhibited strong inhibition on most of the cell line tested. In particular, they demonstrate a mean IC50 of 3.14 and 9.2 g/L in the Hep G2 cell line, respectively.