Synthesis and biological activity of Δ-5, 6-norcantharimides: importance of the 5, 6-bridge

…, JL Scott, J Gilbert, JA Sakoff, A McCluskey

Index: Thaqi, Ali; Scott, Janet L.; Gilbert, Jayne; Sakoff, Jennette A.; McCluskey, Adam European Journal of Medicinal Chemistry, 2010 , vol. 45, # 5 p. 1717 - 1723

Full Text: HTML

Citation Number: 28

Abstract

Cantharidin (1) and norcantharidin (2) are potent protein phosphatase 1 and 2A inhibitors that also display high levels of anticancer activity against a broad range of tumor cells lines. Surprisingly, Δ-5, 6-ethyl norcantharidin (3, cis-tetrahydrofurano [3, 4-c] furan-1, 3-dione) displays neither phosphatase inhibition nor anticancer activity. This suggests that the 5, 6- ethyl bridge is pivotal to both anti-cancer and protein phosphatase activity. Additionally ...