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Synthesis and Evaluation of Millepachine Amino Acid Prodrugs With Enhanced Solubility as Antitumor Agents

A series of amino acid derivatives of millepachine were designed, synthesized, and evaluated for their solubility and antiproliferation ability against tumor. The glycine derivative compound 7a exhibited the best potency and possessed long‐term inhibitory capability on cell viability. It was also confirmed that 7a could arrest the cell cycle at G2/M phase and trigger apoptosis. Furthermore, indirect immunofluorescence staining revealed antitubulin property of 7a, which is consistent with the previously reported derivatives of millepachine. In vivo, 7a suppressed tumor growth in an MDA‐MB‐231 xenograft tumor model. In summary, the exploit of 7a was a successful approach directed by the concept of generating amino acid prodrugs with increased bioavailability.