Cancer metastasis is a major barrier to its treatment and an important cause of patient death. Antimetastatic agents hold promise for patients with advanced metastatic tumors. Aminopeptidase N/CD13 (APN) is being pursued by many as an important target against cancer metastasis and angiogenesis, but there are few reports on the
in vivo evaluation of synthetic APN inhibitors. Herein, a series of compounds targeting APN were synthesized and evaluated for their antimetastasis and antiangiogenesis potency both
in vitro and
in vivo. Excitingly, compounds
4m,
4t, and
4cc, with the most potent APN inhibitory activities, displayed significant antimetastasis and antiangiogenesis effects
in vitro and
in vivo, suggesting that those synthetic APN inhibitors have the potential to overcome cancer metastasis and angiogenesis.
Keywords:
APN/CD13; inhibitors; anticancer; metastasis; angiogenesis