ABT-888, an orally active poly (ADP-ribose) polymerase inhibitor that potentiates DNA-damaging agents in preclinical tumor models
…, Y Luo, Y Luo, TD Penning, JL Bauch, JJ Bouska… - Clinical cancer …, 2007 - AACR
Purpose: To evaluate the preclinical pharmacokinetics and antitumor efficacy of a novel
orally bioavailable poly(ADP-ribose) polymerase (PARP) inhibitor, ABT-888. Experimental …
orally bioavailable poly(ADP-ribose) polymerase (PARP) inhibitor, ABT-888. Experimental …
Discovering novel ligands for macromolecules using X-ray crystallographic screening
…, V Klighofer, JJ Bouska, VL Giranda, J Greer - Nature …, 2000 - nature.com
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, …
at several stages in the process, including genomics/proteomics for target identification, …
Discovery of the Poly(ADP-ribose) Polymerase (PARP) Inhibitor 2-[(R)-2-methylpyrrolidin-2-yl]-1H-benzimidazole-4-carboxamide (ABT-888) for the Treatment of …
…, DJ Frost, V Bontcheva-Diaz, JJ Bouska… - Journal of medicinal …, 2009 - ACS Publications
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 …
inhibitors with a methyl-substituted quaternary center at the point of attachment to the …
Potent and selective inhibitors of Akt kinases slow the progress of tumors in vivo
…, EF Johnson, JD Leverson, JJ Bouska… - Molecular cancer …, 2005 - AACR
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 …
cellular transformation and tumor progression. We report the development of a series of potent …
Preclinical activity of ABT-869, a multitargeted receptor tyrosine kinase inhibitor
…, N Soni, EF Johnson, JO McCall, JJ Bouska… - Molecular cancer …, 2006 - AACR
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 …
of members of the vascular endothelial growth factor (VEGF) and platelet-derived growth …
Discovery of N-(4-(3-Amino-1H-indazol-4-yl)phenyl)-N'-(2-fluoro-5-methylphenyl)urea (ABT-869), a 3-Aminoindazole-Based Orally Active Multitargeted Receptor …
…, DH Albert, JL Bauch, JJ Bouska… - Journal of medicinal …, 2007 - ACS Publications
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-…
as potential anticancer agents, we discovered, through a structure-based design, that 3-…
Thienopyrimidine ureas as novel and potent multitargeted receptor tyrosine kinase inhibitors
…, T Barlozzari, JL Bauch, JJ Bouska… - Journal of medicinal …, 2005 - ACS Publications
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 …
discovered. Investigation of structure−activity relationships at the 5- and 6-positions of the …
Trifluoromethyl ketones as inhibitors of histone deacetylase
…, LJ Pease, KB Glaser, PA Marcotte, JJ Bouska… - Bioorganic & Medicinal …, 2002 - Elsevier
… 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 …
S. Murphy , Steven K. Davidsen … Gong, JH Holms, JJ Bouska, J. Stacey, CK Wada, HR …
Phenoxyphenyl Sulfone N-Formylhydroxylamines (Retrohydroxamates) as Potent, Selective, Orally Bioavailable Matrix Metalloproteinase Inhibitors
…, DH Steinman, DH Albert, JJ Bouska… - Journal of medicinal …, 2002 - ACS Publications
A novel series of sulfone N-formylhydroxylamines (retrohydroxamates) have been investigated
as matrix metalloproteinases (MMP) inhibitors. The substitution of the ether linkage of ABT…
as matrix metalloproteinases (MMP) inhibitors. The substitution of the ether linkage of ABT…
Synthesis and evaluation of a new generation of orally efficacious benzimidazole-based poly (ADP-ribose) polymerase-1 (PARP-1) inhibitors as anticancer agents
Y Tong, JJ Bouska, PA Ellis, EF Johnson… - Journal of medicinal …, 2009 - ACS Publications
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-…
therapeutic agents either capable of sensitizing cytotoxic treatments or acting as stand-…