Fumagillin and Structurally Related Molecules as Source of New Drugs

Diego      Gamba-Sanchez

doi:10.2174/157019312800604724

Abstract

Cancer is one of the most prolific causes of death all around the world. Currently there is a huge focus around the globe on the identification of effective drugs against this disease. One important target is the development of new anti-angiogenic compounds. Fumagillin and other structurally related molecules are some of the most potent anti-angiogenic compounds reported to date with several currently being investigated in clinical studies.

Fumagillin has been used for more than 50 years against microsporidial parasites in animals, however, angiogenesis inhibition constitutes a new activity and an important research topic, this is the reason why nowadays some teams are working to achieve an effective way to obtain fumagillin analogues with more potent anti-angiogenic activity.

Here we present an overview on fumagillin and fumagillin analogues as leads products; we summarize the key structural features for antiangiogenic activity and discuss the total synthesis and synthesis of analogues and their biological activity.

Keywords: Angiogenesis, anti-angiogenic therapy, fumagillin, ovalicin, structure-activity relationship, TNP470, Nosema Apis, Nosema Ceranae, AGM-1470, Plasmodium falciparum, Pollini, Sorensen