Search Results - "BOUSKA, Jennifer"

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 Cancer by Penning, Thomas D, Zhu, Gui-Dong, Gandhi, Viraj B, Gong, Jianchun, Liu, Xuesong, Shi, Yan, Klinghofer, Vered, Johnson, Eric F, Donawho, Cherrie K, Frost, David J, Bontcheva-Diaz, Velitchka, Bouska, Jennifer J, Osterling, Donald J, Olson, Amanda M, Marsh, Kennan C, Luo, Yan, Giranda, Vincent L

“…We have developed a series of cyclic amine-containing benzimidazole carboxamide PARP inhibitors with a methyl-substituted quaternary center at the point of…”
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ABT-888, an Orally Active Poly(ADP-Ribose) Polymerase Inhibitor that Potentiates DNA-Damaging Agents in Preclinical Tumor Models by DONAWHO, Cherrie K, YAN LUO, FERGUSON, Debra C, GHOREISHI-HAACK, Nayereh S, GRIMM, David R, GUAN, Ran, HAN, Edward K, HOLLEY-SHANKS, Rhonda R, HRISTOV, Boris, IDLER, Kenneth B, JARVIS, Ken, JOHNSON, Eric F, YANPING LUO, KLEINBERG, Lawrence R, KLINGHOFER, Vered, LASKO, Loren M, XUESONG LIU, MARSH, Kennan C, MCGONIGAL, Thomas P, MEULBROEK, Jonathan A, OLSON, Amanda M, PALMA, Joann P, RODRIGUEZ, Luis E, PENNING, Thomas D, YAN SHI, STAVROPOULOS, Jason A, TSURUTANI, Alan C, ZHU, Gui-Dong, ROSENBERG, Saul H, GIRANDA, Vincent L, FROST, David J, BAUCH, Joy L, BOUSKA, Jennifer J, BONTCHEVA-DIAZ, Velitchka D, COX, Bryan F, DEWEESE, Theodore L, DILLEHAY, Larry E

“…Purpose: To evaluate the preclinical pharmacokinetics and antitumor efficacy of a novel orally bioavailable poly(ADP-ribose) polymerase (PARP) inhibitor,…”
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Synthesis and SAR of novel tricyclic quinoxalinone inhibitors of poly(ADP-ribose)polymerase-1 (PARP-1) by Miyashiro, Julie, Woods, Keith W., Park, Chang H., Liu, Xuesong, Shi, Yan, Johnson, Eric F., Bouska, Jennifer J., Olson, Amanda M., Luo, Yan, Fry, Elizabeth H., Giranda, Vincent L., Penning, Thomas D.

“…Based on screening hit 1, a series of tricyclic quinoxalinones have been designed and evaluated for inhibition of PARP-1. Substitutions at the 7- and…”
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A quantitation method for mass spectrometry imaging by Koeniger, Stormy L., Talaty, Nari, Luo, Yanping, Ready, Damien, Voorbach, Martin, Seifert, Terese, Cepa, Steve, Fagerland, Jane A., Bouska, Jennifer, Buck, Wayne, Johnson, Robert W., Spanton, Stephen

“…A new quantitation method for mass spectrometry imaging (MSI) with matrix‐assisted laser desorption/ionization (MALDI) has been developed. In this method, drug…”
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Synthesis and Evaluation of a New Generation of Orally Efficacious Benzimidazole-Based Poly(ADP-ribose) Polymerase-1 (PARP-1) Inhibitors as Anticancer Agents by Tong, Yunsong, Bouska, Jennifer J, Ellis, Paul A, Johnson, Eric F, Leverson, Joel, Liu, Xuesong, Marcotte, Patrick A, Olson, Amanda M, Osterling, Donald J, Przytulinska, Magdalena, Rodriguez, Luis E, Shi, Yan, Soni, Nirupama, Stavropoulos, Jason, Thomas, Sheela, Donawho, Cherrie K, Frost, David J, Luo, Yan, Giranda, Vincent L, Penning, Thomas D

“…Small molecule inhibitors of PARP-1 have been pursued by various organizations as potential therapeutic agents either capable of sensitizing cytotoxic…”
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Potent and selective inhibitors of Akt kinases slow the progress of tumors in vivo by Luo, Yan, Shoemaker, Alexander R, Liu, Xuesong, Woods, Keith W, Thomas, Sheela A, de Jong, Ron, Han, Edward K, Li, Tongmei, Stoll, Vincent S, Powlas, Jessica A, Oleksijew, Anatol, Mitten, Michael J, Shi, Yan, Guan, Ran, McGonigal, Thomas P, Klinghofer, Vered, Johnson, Eric F, Leverson, Joel D, Bouska, Jennifer J, Mamo, Mulugeta, Smith, Richard A, Gramling-Evans, Emily E, Zinker, Bradley A, Mika, Amanda K, Nguyen, Phong T, Oltersdorf, Tilman, Rosenberg, Saul H, Li, Qun, Giranda, Vincent L

“…The Akt kinases are central nodes in signal transduction pathways that are important for cellular transformation and tumor progression. We report the…”
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Preclinical activity of ABT-869, a multitargeted receptor tyrosine kinase inhibitor by Albert, Daniel H, Tapang, Paul, Magoc, Terrance J, Pease, Lori J, Reuter, David R, Wei, Ru-Qi, Li, Junling, Guo, Jun, Bousquet, Peter F, Ghoreishi-Haack, Nayereh S, Wang, Baole, Bukofzer, Gail T, Wang, Yi-Chun, Stavropoulos, Jason A, Hartandi, Kresna, Niquette, Amanda L, Soni, Nirupama, Johnson, Eric F, McCall, J Owen, Bouska, Jennifer J, Luo, Yanping, Donawho, Cherrie K, Dai, Yujia, Marcotte, Patrick A, Glaser, Keith B, Michaelides, Michael R, Davidsen, Steven K

“…ABT-869 is a structurally novel, receptor tyrosine kinase (RTK) inhibitor that is a potent inhibitor of members of the vascular endothelial growth factor…”
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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 Tyrosine Kinase Inhibitor by Dai, Yujia, Hartandi, Kresna, Ji, Zhiqin, Ahmed, Asma A, Albert, Daniel H, Bauch, Joy L, Bouska, Jennifer J, Bousquet, Peter F, Cunha, George A, Glaser, Keith B, Harris, Christopher M, Hickman, Dean, Guo, Jun, Li, Junling, Marcotte, Patrick A, Marsh, Kennan C, Moskey, Maria D, Martin, Ruth L, Olson, Amanda M, Osterling, Donald J, Pease, Lori J, Soni, Niru B, Stewart, Kent D, Stoll, Vincent S, Tapang, Paul, Reuter, David R, Davidsen, Steven K, Michaelides, Michael R

“…In our continued efforts to search for potent and novel receptor tyrosine kinase (RTK) inhibitors as potential anticancer agents, we discovered, through a…”
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Discovering novel ligands for macromolecules using X-ray crystallographic screening by Nienaber, Vicki L, Richardson, Paul L, Klighofer, Vered, Bouska, Jennifer J, Giranda, Vincent L, Greer, Jonathan

“…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…”
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Discovery of potent and selective thienopyrimidine inhibitors of Aurora kinases by McClellan, William J., Dai, Yujia, Abad-Zapatero, Cele, Albert, Daniel H., Bouska, Jennifer J., Glaser, Keith B., Magoc, Terry J., Marcotte, Patrick A., Osterling, Donald J., Stewart, Kent D., Davidsen, Steven K., Michaelides, Michael R.

“…In an effort to discover Aurora kinase inhibitors, an HTS hit revealed an amide containing pyrrolopyrimidine compound. Replacement of the pyrrolopyrimidine…”
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Discovery of 3H-Benzo[4,5]thieno[3,2-d]pyrimidin-4-ones as Potent, Highly Selective, and Orally Bioavailable Inhibitors of the Human Protooncogene Proviral Insertion Site in Moloney Murine Leukemia Virus (PIM) Kinases by Tao, Zhi-Fu, Hasvold, Lisa A, Leverson, Joel D, Han, Edward K, Guan, Ran, Johnson, Eric F, Stoll, Vincent S, Stewart, Kent D, Stamper, Geoff, Soni, Nirupama, Bouska, Jennifer J, Luo, Yan, Sowin, Thomas J, Lin, Nan-Horng, Giranda, Vincent S, Rosenberg, Saul H, Penning, Thomas D

“…Pim-1, Pim-2, and Pim-3 are a family of serine/threonine kinases which have been found to be overexpressed in a variety of hematopoietic malignancies and solid…”
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Discovery and SAR of orally efficacious tetrahydropyridopyridazinone PARP inhibitors for the treatment of cancer by Zhu, Gui-Dong, Gong, Jianchun, Gandhi, Viraj B., Liu, Xuesong, Shi, Yan, Johnson, Eric F., Donawho, Cherrie K., Ellis, Paul A, Bouska, Jennifer J., Osterling, Donald J., Olson, Amanda M., Park, Chang, Luo, Yan, Shoemaker, Alexander, Giranda, Vincent L., Penning, Thomas D.

“…PARP-1, the most abundant member of the PARP superfamily of nuclear enzymes, has emerged as a promising molecular target in the past decade particularly for…”
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ABT-869, a multitargeted receptor tyrosine kinase inhibitor: inhibition of FLT3 phosphorylation and signaling in acute myeloid leukemia by Shankar, Deepa B., Li, Junling, Tapang, Paul, Owen McCall, J., Pease, Lori J., Dai, Yujia, Wei, Ru-Qi, Albert, Daniel H., Bouska, Jennifer J., Osterling, Donald J., Guo, Jun, Marcotte, Patrick A., Johnson, Eric F., Soni, Niru, Hartandi, Kresna, Michaelides, Michael R., Davidsen, Steven K., Priceman, Saul J., Chang, Jenny C., Rhodes, Katrin, Shah, Neil, Moore, Theodore B., Sakamoto, Kathleen M., Glaser, Keith B.

“…In 15% to 30% of patients with acute myeloid leukemia (AML), aberrant proliferation is a consequence of a juxtamembrane mutation in the FLT3 gene (FMS-like…”
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Discovery and SAR of 2-(1-propylpiperidin-4-yl)-1H-benzimidazole-4-carboxamide: A potent inhibitor of poly(ADP-ribose) polymerase (PARP) for the treatment of cancer by Penning, Thomas D, Zhu, Gui-Dong, Gandhi, Viraj B, Gong, Jianchun, Thomas, Sheela, Lubisch, Wilfried, Grandel, Roland, Wernet, Wolfgang, Park, Chang H, Fry, Elizabeth H, Liu, Xuesong, Shi, Yan, Klinghofer, Vered, Johnson, Eric F, Donawho, Cherrie K, Frost, David J, Bontcheva-Diaz, Velitchka, Bouska, Jennifer J, Olson, Amanda M, Marsh, Kennan C, Luo, Yan, Rosenberg, Saul H, Giranda, Vincent L

“…We have developed a series of cyclic amine-containing benzimidazole carboxamide poly(ADP-ribose)polymerase (PARP) inhibitors, with good PARP-1 enzyme potency,…”
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7-Aminopyrazolo[1,5-a]pyrimidines as Potent Multitargeted Receptor Tyrosine Kinase Inhibitors by Frey, Robin R, Curtin, Michael L, Albert, Daniel H, Glaser, Keith B, Pease, Lori J, Soni, Niru B, Bouska, Jennifer J, Reuter, David, Stewart, Kent D, Marcotte, Patrick, Bukofzer, Gail, Li, Junling, Davidsen, Steven K, Michaelides, Michael R

“…7-Aminopyrazolo[1,5-a]pyrimidine urea receptor tyrosine kinase inhibitors have been discovered. Investigation of structure−activity relationships of the…”
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Preclinical characterization of ABT-348, a kinase inhibitor targeting the aurora, vascular endothelial growth factor receptor/platelet-derived growth factor receptor, and Src kinase families by Glaser, Keith B, Li, Junling, Marcotte, Patrick A, Magoc, Terrance J, Guo, Jun, Reuter, David R, Tapang, Paul, Wei, Ru-Qi, Pease, Lori J, Bui, Mai H, Chen, Zehan, Frey, Robin R, Johnson, Eric F, Osterling, Donald J, Olson, Amanda M, Bouska, Jennifer J, Luo, Yanping, Curtin, Michael L, Donawho, Cherrie K, Michaelides, Michael R, Tse, Chris, Davidsen, Steven K, Albert, Daniel H

“…ABT-348 [1-(4-(4-amino-7-(1-(2-hydroxyethyl)-1H-pyrazol-4-yl)thieno[3,2-c]pyridin-3-yl)phenyl)-3-(3-fluorophenyl)urea] is a novel ATP-competitive multitargeted…”
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The PARP Inhibitor, ABT-888 Potentiates Temozolomide: Correlation with Drug Levels and Reduction in PARP Activity In Vivo by PALMA, Joann P, RODRIGUEZ, Luis E, XUESONG LIU, OLSON, Amanda, SALTARELLI, Mary J, YAN SHI, STAVROPOULOS, Jason A, ZHU, Gui-Dong, PENNING, Thomas D, YAN LUO, GIRANDA, Vincent L, ROSENBERG, Saul H, BONTCHEVA-DIAZ, Velitchka D, FROST, David J, DONAWHO, Cherrie K, BOUSKA, Jennifer J, BUKOFZER, Gail, COLON-LOPEZ, Milagros, RAN GUAN, JARVIS, Kenneth, JOHNSON, Eric F, KLINGHOFER, Vered

“…ABT-888 is a potent, orally bioavailable PARP-1/-2 inhibitor shown to potentiate DNA damaging agents. The ability to potentiate temozolomide (TMZ) and develop…”
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Synthesis and SAR of indazole-pyridine based protein kinase B/Akt inhibitors by Woods, Keith W., Fischer, John P., Claiborne, Akiyo, Li, Tongmei, Thomas, Sheela A., Zhu, Gui-Dong, Diebold, Robert B., Liu, Xuesong, Shi, Yan, Klinghofer, Vered, Han, Edward K., Guan, Ran, Magnone, Shayna R., Johnson, Eric F., Bouska, Jennifer J., Olson, Amanda M., Jong, Ron de, Oltersdorf, Tilman, Luo, Yan, Rosenberg, Saul H., Giranda, Vincent L., Li, Qun

“…SAR studies leading from the isoquinoline analogue to the discovery of the indazole moiety are described. A series of heteroaryl-pyridine containing inhibitors…”
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Thienopyridine ureas as dual inhibitors of the VEGF and Aurora kinase families by Curtin, Michael L., Frey, Robin R., Heyman, H. Robin, Soni, Niru B., Marcotte, Patrick A., Pease, Lori J., Glaser, Keith B., Magoc, Terrance J., Tapang, Paul, Albert, Daniel H., Osterling, Donald J., Olson, Amanda M., Bouska, Jennifer J., Guan, Zhiwen, Preusser, Lee C., Polakowski, James S., Stewart, Kent D., Tse, Chris, Davidsen, Steven K., Michaelides, Michael R.

“…A series of thienopyridine ureas with dual inhibitory activity against KDR and Aurora B kinase has been identified. Compound 2 (ABT-348) of this series is…”
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Design, Synthesis, and Biological Activity of 5,10-Dihydro-dibenzo[b,e][1,4]diazepin-11-one-Based Potent and Selective Chk-1 Inhibitors by Wang, Le, Sullivan, Gerard M, Hexamer, Laura A, Hasvold, Lisa A, Thalji, Reema, Przytulinska, Magdalena, Tao, Zhi-Fu, Li, Gaoquan, Chen, Zehan, Xiao, Zhan, Gu, Wen-Zhen, Xue, John, Bui, Mai-Ha, Merta, Philip, Kovar, Peter, Bouska, Jennifer J, Zhang, Haiying, Park, Chang, Stewart, Kent D, Sham, Hing L, Sowin, Thomas J, Rosenberg, Saul H, Lin, Nan-Horng

“…A novel series of 5,10-dihydro-dibenzo[b,e][1,4]diazepin-11-ones have been synthesized as potent and selective checkpoint kinase 1 (Chk1) inhibitors via…”
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