Integrins are cell surface receptors that take part in cell – cell adhesion and cell – extracellular matrix (ECM) adhesion events as well as in cell migration and cell signaling. ?5?1 integrins are expressed on a wide range among brain tumor cells. In this study, an intermediate spiroisoxazolinopyrrole of the most specific ?5?1 integrin antagonist SJ749 was synthesized. Fischer esterification reaction, Swern oxidation, and Wittig olefination were performed. Next, fluorinated diaminopropionate molecules were synthesized for coupling to SJ749 instead of the (2,4,6-trimethylphenyl) diaminopropionate. Finally, the biological evaluation of the molecules synthesized was performed. These assays included cytotoxicity and cell proliferation.