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Published in Journal of pharmaceutical sciences (03.10.2024)
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A novel CDK9 inhibitor increases the efficacy of venetoclax (ABT-199) in multiple models of hematologic malignancies
Phillips, Darren C., Jin, Sha, Gregory, Gareth P., Zhang, Qi, Xue, John, Zhao, Xiaoxian, Chen, Jun, Tong, Yunsong, Zhang, Haichao, Smith, Morey, Tahir, Stephen K., Clark, Rick F., Penning, Thomas D., Devlin, Jennifer R., Shortt, Jake, Hsi, Eric D., Albert, Daniel H., Konopleva, Marina, Johnstone, Ricky W., Leverson, Joel D., Souers, Andrew J.
Published in Leukemia (01.06.2020)
Published in Leukemia (01.06.2020)
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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
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
Published in Journal of medicinal chemistry (22.01.2009)
Published in Journal of medicinal chemistry (22.01.2009)
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Discovery of Potent Azetidine-Benzoxazole MerTK Inhibitors with In Vivo Target Engagement
Frey, Robin R., Jana, Navendu, Gorman, Jacob V., Wang, Jin, Smith, Heath A., Bromberg, Kenneth D., Thakur, Ashish, Doktor, Stella Z., Indulkar, Anura S., Jakob, Clarissa G., Upadhyay, Anup K., Qiu, Wei, Manaves, Vlasios, Gambino, Frank, Valentino, Stephen A., Montgomery, Debra, Zhou, Yebin, Li, Tao, Buchanan, Fritz G., Ferguson, Debra C., Kurnick, Matthew D., Kapecki, Nicolas, Lai, Albert, Michaelides, Michael R., Penning, Thomas D.
Published in Journal of medicinal chemistry (10.10.2024)
Published in Journal of medicinal chemistry (10.10.2024)
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Iniparib Nonselectively Modifies Cysteine-Containing Proteins in Tumor Cells and Is Not a Bona Fide PARP Inhibitor
XUESONG LIU, YAN SHI, XU, Allison J, LAYER, Ramesh, HARLAN, John E, SOLOMON, Larry R, DONAWHO, Cherrie K, PENNING, Thomas D, JOHNSON, Eric F, SHOEMAKER, Alexander R, MAAG, David X, PALMA, Joann P, PATTERSON, Melanie J, ELLIS, Paul A, SURBER, Bruce W, READY, Damien B, SONI, Niru B, LADROR, Uri S
Published in Clinical cancer research (15.01.2012)
Published in Clinical cancer research (15.01.2012)
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Discovery of A‑910, a Highly Potent and Orally Bioavailable Dual MerTK/Axl-Selective Tyrosine Kinase Inhibitor
Yu, Yiyun, Jang, Miyeon, Miyashiro, Julie, Clark, Richard F., Zhu, Gui-Dong, Gong, Jane, Dai, Yujia, Frey, Robin R., Penning, Thomas D., Kim, Hadong, Lee, Hyung Ki, Kim, Jin Kwan, Ryu, Ki Moon, Park, Seong Jin, Yoon, Taeyoung, Li, Tao, Kurnick, Matthew D., Kapecki, Nicolas J., Li, Leiming, Gorman, Jacob V., Montgomery, Debra A., Manaves, Vlasios, Bromberg, Kenneth D., Doktor, Stella Z., Thakur, Ashish, Wang, Jin, Smith, Heath A., Buchanan, Fritz G., Ferguson, Debra C., Torrent, Maricel, Jakob, Clarissa G., Qiu, Wei, Upadhyay, Anup K., Martin, Ruth L., Lai, Albert, Michaelides, Michael R.
Published in Journal of medicinal chemistry (10.10.2024)
Published in Journal of medicinal chemistry (10.10.2024)
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ABT-888 Confers Broad In vivo Activity in Combination with Temozolomide in Diverse Tumors
PALMA, Joann P, WANG, Yi-Chun, ZHU, Gui-Dong, PENNING, Thomas D, GIRANDA, Vincent L, ROSENBERG, Saul H, FROST, David J, DONAWHO, Cherrie K, RODRIGUEZ, Luis E, MONTGOMERY, Debra, ELLIS, Paul A, BUKOFZER, Gail, NIQUETTE, Amanda, XUESONG LIU, YAN SHI, LASKO, Loren
Published in Clinical cancer research (01.12.2009)
Published in Clinical cancer research (01.12.2009)
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Corrigendum to “Investigation of biaryl heterocycles as inhibitors of Wee1 kinase” [Bioorg. Med. Chem. Lett. 29 (2019) 1481–1486]
Mastracchio, Anthony, Lai, Chunqiu, Torrent, Maricel, Bromberg, Kenneth, Buchanan, Fritz G., Ferguson, Debra, Bontcheva, Velitchka, Johnson, Eric F., Lasko, Loren, Maag, David, Shoemaker, Alexander R., Penning, Thomas D.
Published in Bioorganic & medicinal chemistry letters (15.02.2020)
Published in Bioorganic & medicinal chemistry letters (15.02.2020)
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Investigation of biaryl heterocycles as inhibitors of Wee1 kinase
Mastracchio, Anthony, Lai, Chunqiu, Torrent, Maricel, Bromberg, Kenneth, Buchanan, Fritz G., Ferguson, Debra, Bontcheva, Velitchka, Johnson, Eric F., Lasko, Loren, Maag, David, Shoemaker, Alexander R., Penning, Thomas D.
Published in Bioorganic & medicinal chemistry letters (15.06.2019)
Published in Bioorganic & medicinal chemistry letters (15.06.2019)
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Synthesis and SAR of novel tricyclic quinoxalinone inhibitors of poly(ADP-ribose)polymerase-1 (PARP-1)
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.
Published in Bioorganic & medicinal chemistry letters (01.08.2009)
Published in Bioorganic & medicinal chemistry letters (01.08.2009)
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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
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
Published in Journal of medicinal chemistry (12.11.2009)
Published in Journal of medicinal chemistry (12.11.2009)
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Balancing Properties with Carboxylates: A Lead Optimization Campaign for Selective and Orally Active CDK9 Inhibitors
Tong, Yunsong, Florjancic, Alan S, Clark, Rick F, Lai, Chunqiu, Mastracchio, Anthony, Zhu, Gui-dong, Smith, Morey L, Kovar, Peter J, Shaw, Bailin, Albert, Daniel H, Qiu, Wei, Longenecker, Kenton L, Liu, Xiaoqin, Olson, Amanda M, Osterling, Donald J, Tahir, Stephen K, Phillips, Darren C, Leverson, Joel D, Souers, Andrew J, Penning, Thomas D
Published in ACS medicinal chemistry letters (08.07.2021)
Published in ACS medicinal chemistry letters (08.07.2021)
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Acquired Resistance to Combination Treatment with Temozolomide and ABT-888 Is Mediated by Both Base Excision Repair and Homologous Recombination DNA Repair Pathways
Liu, Xuesong, Han, Edward K, Anderson, Mark, Shi, Yan, Semizarov, Dimitri, Wang, Gang, McGonigal, Thomas, Roberts, Lisa, Lasko, Loren, Palma, Joann, Zhu, Gui-Dong, Penning, Thomas, Rosenberg, Saul, Giranda, Vincent L, Luo, Yan, Leverson, Joel, Johnson, Eric F, Shoemaker, Alexander R
Published in Molecular cancer research (01.10.2009)
Published in Molecular cancer research (01.10.2009)
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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
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
Published in Journal of medicinal chemistry (12.11.2009)
Published in Journal of medicinal chemistry (12.11.2009)
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Discovery and SAR of orally efficacious tetrahydropyridopyridazinone PARP inhibitors for the treatment of cancer
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.
Published in Bioorganic & medicinal chemistry (01.08.2012)
Published in Bioorganic & medicinal chemistry (01.08.2012)
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Structural basis for selective inhibition of cyclooxygenase-2 by anti-inflammatory agents
Kurumbail, Ravi G, Stevens, Anna M, Gierse, James K, McDonald, Joseph J, Stegeman, Roderick A, Pak, Jina Y, Gildehaus, Daniel, iyashiro, Julie M, Penning, Thomas D, Seibert, Karen, Isakson, Peter C, Stallings, William C
Published in Nature (London) (26.12.1996)
Published in Nature (London) (26.12.1996)
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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
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
Published in Bioorganic & medicinal chemistry (15.07.2008)
Published in Bioorganic & medicinal chemistry (15.07.2008)
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Isoxazolo[3,4- b]quinoline-3,4(1H,9H)-diones as unique, potent and selective inhibitors for Pim-1 and Pim-2 kinases: Chemistry, biological activities, and molecular modeling
Tong, Yunsong, Stewart, Kent D., Thomas, Sheela, Przytulinska, Magdalena, Johnson, Eric F., Klinghofer, Vered, Leverson, Joel, McCall, Owen, Soni, Niru B., Luo, Yan, Lin, Nan-horng, Sowin, Thomas J., Giranda, Vincent L., Penning, Thomas D.
Published in Bioorganic & medicinal chemistry (01.10.2008)
Published in Bioorganic & medicinal chemistry (01.10.2008)
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Potentiation of Temozolomide Cytotoxicity by Poly(ADP)Ribose Polymerase Inhibitor ABT-888 Requires a Conversion of Single-Stranded DNA Damages to Double-Stranded DNA Breaks
Liu, Xuesong, Shi, Yan, Guan, Ran, Donawho, Cherrie, Luo, Yanping, Palma, Joann, Zhu, Gui-Dong, Johnson, Eric F, Rodriguez, Luis E, Ghoreishi-Haack, Nayereh, Jarvis, Ken, Hradil, Vincent P, Colon-Lopez, Milagros, Cox, Bryan F, Klinghofer, Vered, Penning, Thomas, Rosenberg, Saul H, Frost, David, Giranda, Vincent L, Luo, Yan
Published in Molecular cancer research (01.10.2008)
Published in Molecular cancer research (01.10.2008)
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Discovery and SAR of substituted 3-oxoisoindoline-4-carboxamides as potent inhibitors of poly(ADP-ribose) polymerase (PARP) for the treatment of cancer
Gandhi, Viraj B., Luo, Yan, Liu, Xuesong, Shi, Yan, Klinghofer, Vered, Johnson, Eric F., Park, Chang, Giranda, Vincent L., Penning, Thomas D., Zhu, Gui-Dong
Published in Bioorganic & medicinal chemistry letters (01.02.2010)
Published in Bioorganic & medicinal chemistry letters (01.02.2010)
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