Ontology highlight
ABSTRACT:
SUBMITTER: Zhang Y
PROVIDER: S-EPMC4499820 | biostudies-other | 2015 Jul
REPOSITORIES: biostudies-other
Zhang Yong Y Seigal Benjamin A BA Terrett Nicholas K NK Talbott Randy L RL Fargnoli Joseph J Naglich Joseph G JG Chaudhry Charu C Posy Shana L SL Vuppugalla Ragini R Cornelius Georgia G Lei Ming M Wang Chunlei C Zhang Yingru Y Schmidt Robert J RJ Wei Donna D DD Miller Michael M MM Allen Martin P MP Li Ling L Carter Percy H PH Vite Gregory D GD Borzilleri Robert M RM
ACS medicinal chemistry letters 20150527 7
A series of dimeric macrocyclic compounds were prepared and evaluated as antagonists for inhibitor of apoptosis proteins. The most potent analogue 11, 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 11 demonstrated significant antitumor activity in the A875 human melanoma xenograft model at doses as low as 2 m ...[more]