




Benzimidazole Series: The benzimidazole analog
series represents a group of about 20 novel small molecules with distinct
structures from previous benzimidazoles that
expressed tubulin binding activity in yeast and mammalian cells. The new
analogs (the AMP-500 series) are small molecules (< 500MW), synthesized in
AmpliMed's
laboratory under Professor Remers direction. Design criteria involved good
water solubility and unique structures from prior benzimidazole agents. Some
of these analogs
have shown anti-tumor efficacy in vitro against human tumor cell lines. A
lead analog, AMP-507, has been selected for further preclinical development
based on its favorable
activity profile in preclinical experimental tumor models. Preliminary
mechanism of action studies suggest that these newer analogs have a actions
that are distinct from prior
benzimidazoles used as anticancer agents.