1 research outputs found
Dimeric Macrocyclic Antagonists of Inhibitor of Apoptosis Proteins for the Treatment of Cancer
A series of dimeric macrocyclic compounds
were prepared and evaluated
as antagonists for inhibitor of apoptosis proteins. The most potent
analogue <b>11</b>, which binds to XIAP and c-IAP proteins with
high affinity and induces caspase-3 activation and ultimately cell
apoptosis, inhibits growth of human melanoma and colorectal cell lines
at low nanomolar concentrations. Furthermore, compound <b>11</b> demonstrated significant antitumor activity in the A875 human melanoma
xenograft model at doses as low as 2 mg/kg on a q3d schedule