NPI-2358 is a tubulin-depolymerizing agent: in-vitro evidence for activity as a tumor vascular-disrupting agent

B Nicholson, GK Lloyd, BR Miller, MA Palladino… - Anti-cancer …, 2006 - journals.lww.com
The diketopiperazine NPI-2358 is a synthetic analog of NPI-2350, a natural product isolated
from Aspergillus sp., which depolymerizes microtubules in A549 human lung carcinoma
cells. Although structurally different from the colchicine-binding site agents reported to date,
NPI-2358 binds to the colchicine-binding site of tubulin. NPI-2358 has potent in-vitro anti-
tumor activity against various human tumor cell lines and maintains activity against tumor
cell lines with various multidrug-resistant (MDR) profiles. In addition, when evaluated in …