Purpose: To evaluate the preclinical pharmacokinetics and antitumor efficacy of a novel
orally bioavailable poly(ADP-ribose) polymerase (PARP) inhibitor, ABT-888. Experimental …

The need to decrease the time scale for clinical compound discovery has led to innovations
at several stages in the process, including genomics/proteomics for target identification, …

We have developed a series of cyclic amine-containing benzimidazole carboxamide PARP
inhibitors with a methyl-substituted quaternary center at the point of attachment to the …

The Akt kinases are central nodes in signal transduction pathways that are important for
cellular transformation and tumor progression. We report the development of a series of potent …

ABT-869 is a structurally novel, receptor tyrosine kinase (RTK) inhibitor that is a potent inhibitor
of members of the vascular endothelial growth factor (VEGF) and platelet-derived growth …

In our continued efforts to search for potent and novel receptor tyrosine kinase (RTK) inhibitors
as potential anticancer agents, we discovered, through a structure-based design, that 3-…

A series of novel thienopyrimidine-based receptor tyrosine kinase inhibitors has been
discovered. Investigation of structure−activity relationships at the 5- and 6-positions of the …

… Michaelides , Junling Li , Lori J. Pease , Keith B. Glaser , Patrick A. … Bouska , Shannon
S. Murphy , Steven K. Davidsen … Gong, JH Holms, JJ Bouska, J. Stacey, CK Wada, HR …

A novel series of sulfone N-formylhydroxylamines (retrohydroxamates) have been investigated
as matrix metalloproteinases (MMP) inhibitors. The substitution of the ether linkage of ABT…

Small molecule inhibitors of PARP-1 have been pursued by various organizations as potential
therapeutic agents either capable of sensitizing cytotoxic treatments or acting as stand-…