Discovery of N‑Ethyl-4-[2-(4-fluoro-2,6-dimethyl-phenoxy)-5-(1-hydroxy-1-methyl-ethyl)phenyl]-6-methyl-7-oxo‑1H‑pyrrolo[2,3‑c]pyridine-2-carboxamide (ABBV-744), a BET Bromodomain Inhibitor with Selectivity for the Second Bromodomain
Sheppard, George S, Wang, Le, Fidanze, Steven D, Hasvold, Lisa A, Liu, Dachun, Pratt, John K, Park, Chang H, Longenecker, Kenton, Qiu, Wei, Torrent, Maricel, Kovar, Peter J, Bui, Mai, Faivre, Emily, Huang, Xiaoli, Lin, Xiaoyu, Wilcox, Denise, Zhang, Lu, Shen, Yu, Albert, Daniel H, Magoc, Terrance J, Rajaraman, Ganesh, Kati, Warren M, McDaniel, Keith F
Published in Journal of medicinal chemistry (28.05.2020)
Published in Journal of medicinal chemistry (28.05.2020)
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Discovery of N -Ethyl-4-[2-(4-fluoro-2,6-dimethyl-phenoxy)-5-(1-hydroxy-1-methyl-ethyl)phenyl]-6-methyl-7-oxo-1 H -pyrrolo[2,3- c ]pyridine-2-carboxamide (ABBV-744), a BET Bromodomain Inhibitor with Selectivity for the Second Bromodomain
Sheppard, George S, Wang, Le, Fidanze, Steven D, Hasvold, Lisa A, Liu, Dachun, Pratt, John K, Park, Chang H, Longenecker, Kenton, Qiu, Wei, Torrent, Maricel, Kovar, Peter J, Bui, Mai, Faivre, Emily, Huang, Xiaoli, Lin, Xiaoyu, Wilcox, Denise, Zhang, Lu, Shen, Yu, Albert, Daniel H, Magoc, Terrance J, Rajaraman, Ganesh, Kati, Warren M, McDaniel, Keith F
Published in Journal of medicinal chemistry (28.05.2020)
Published in Journal of medicinal chemistry (28.05.2020)
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Therapeutic Implications for the Induced Levels of Chk1 in Myc-Expressing Cancer Cells
HÖGLUND, Andreas, NILSSON, Lisa M, VEPPIL MURALIDHARAN, Somsundar, HASVOLD, Lisa A, MERTA, Philip, RUDELIUS, Martina, NIKOLOVA, Viktoriya, KELLER, Ulrich, NILSSON, Jonas A
Published in Clinical cancer research (15.11.2011)
Published in Clinical cancer research (15.11.2011)
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Discovery of N‑(4-(2,4-Difluorophenoxy)-3-(6-methyl-7-oxo-6,7-dihydro‑1H‑pyrrolo[2,3‑c]pyridin-4-yl)phenyl)ethanesulfonamide (ABBV-075/Mivebresib), a Potent and Orally Available Bromodomain and Extraterminal Domain (BET) Family Bromodomain Inhibitor
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Published in Journal of medicinal chemistry (26.10.2017)
Published in Journal of medicinal chemistry (26.10.2017)
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Fragment-Based, Structure-Enabled Discovery of Novel Pyridones and Pyridone Macrocycles as Potent Bromodomain and Extra-Terminal Domain (BET) Family Bromodomain Inhibitors
Wang, Le, Pratt, John K, Soltwedel, Todd, Sheppard, George S, Fidanze, Steven D, Liu, Dachun, Hasvold, Lisa A, Mantei, Robert A, Holms, James H, McClellan, William J, Wendt, Michael D, Wada, Carol, Frey, Robin, Hansen, T. Matthew, Hubbard, Robert, Park, Chang H, Li, Leiming, Magoc, Terrance J, Albert, Daniel H, Lin, Xiaoyu, Warder, Scott E, Kovar, Peter, Huang, Xiaoli, Wilcox, Denise, Wang, Rongqi, Rajaraman, Ganesh, Petros, Andrew M, Hutchins, Charles W, Panchal, Sanjay C, Sun, Chaohong, Elmore, Steven W, Shen, Yu, Kati, Warren M, McDaniel, Keith F
Published in Journal of medicinal chemistry (11.05.2017)
Published in Journal of medicinal chemistry (11.05.2017)
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Discovery and optimization of novel constrained pyrrolopyridone BET family inhibitors
Fidanze, Steven D., Liu, Dachun, Mantei, Robert A., Hasvold, Lisa A., Pratt, John K., Sheppard, George S., Wang, Le, Holms, James H., Dai, Yujia, Aguirre, Ana, Bogdan, Andrew, Dietrich, Justin D., Marjanovic, Jasmina, Park, Chang H., Hutchins, Charles W., Lin, Xiaoyu, Bui, Mai H., Huang, Xiaoli, Wilcox, Denise, Li, Leiming, Wang, Rongqi, Kovar, Peter, Magoc, Terrance J., Rajaraman, Ganesh, Albert, Daniel H., Shen, Yu, Kati, Warren M., McDaniel, Keith F.
Published in Bioorganic & medicinal chemistry letters (01.06.2018)
Published in Bioorganic & medicinal chemistry letters (01.06.2018)
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Methylpyrrole inhibitors of BET bromodomains
Hasvold, Lisa A., Sheppard, George S., Wang, Le, Fidanze, Steven D., Liu, Dachun, Pratt, John K., Mantei, Robert A., Wada, Carol K., Hubbard, Robbert, Shen, Yu, Lin, Xiaoyu, Huang, Xiaoli, Warder, Scott E., Wilcox, Denise, Li, Leiming, Buchanan, F. Greg, Smithee, Lauren, Albert, Daniel H., Magoc, Terrance J., Park, Chang H., Petros, Andrew M., Panchal, Sanjay C., Sun, Chaohong, Kovar, Peter, Soni, Nirupama B., Elmore, Steven W., Kati, Warren M., McDaniel, Keith F.
Published in Bioorganic & medicinal chemistry letters (15.05.2017)
Published in Bioorganic & medicinal chemistry letters (15.05.2017)
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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)
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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
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Published in Journal of medicinal chemistry (23.08.2007)
Published in Journal of medicinal chemistry (23.08.2007)
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Palladium(II)-Catalyzed Cyclization of Olefinic Tosylamides
Larock, Richard C, Hightower, Timothy R, Hasvold, Lisa A, Peterson, Karl P
Published in Journal of organic chemistry (31.05.1996)
Published in Journal of organic chemistry (31.05.1996)
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Synthesis and biological evaluation of 1-(2,4,5-trisubstituted phenyl)-3-(5-cyanopyrazin-2-yl)ureas as potent Chk1 kinase inhibitors
Li, Gaoquan, Hasvold, Lisa A., Tao, Zhi-Fu, Wang, Gary T., Gwaltney, Stephen L., Patel, Jyoti, Kovar, Peter, Credo, Robert B., Chen, Zehan, Zhang, Haiying, Park, Chang, Sham, Hing L., Sowin, Thomas, Rosenberg, Saul H., Lin, Nan-Horng
Published in Bioorganic & medicinal chemistry letters (15.04.2006)
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Investigation of novel 7,8-disubstituted-5,10-dihydro-dibenzo[ b, e][1,4]diazepin-11-ones as potent Chk1 inhibitors
Hasvold, Lisa A., Wang, Le, Przytulinska, Magdalena, Xiao, Zhan, Chen, Zehan, Gu, Wen-Zhen, Merta, Philip J., Xue, John, Kovar, Peter, Zhang, Haiying, Park, Chang, Sowin, Thomas J., Rosenberg, Saul H., Lin, Nan-Horng
Published in Bioorganic & medicinal chemistry (01.04.2008)
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Design and synthesis of o-trifluoromethylbiphenyl substituted 2-amino-nicotinonitriles as inhibitors of farnesyltransferase
Wang, Gary T., Wang, Xilu, Wang, Weibo, Hasvold, Lisa A., Sullivan, Gerry, Hutchins, Charles W., O’Conner, Steve, Gentiles, Robert, Sowin, Thomas, Cohen, Jerry, Gu, Wen-Zhen, Zhang, Haiying, Rosenberg, Saul H., Sham, Hing L.
Published in Bioorganic & medicinal chemistry letters (03.01.2005)
Published in Bioorganic & medicinal chemistry letters (03.01.2005)
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Aryl tetrahydropyridine inhibitors of farnesyltransferase: glycine, phenylalanine and histidine derivatives
Gwaltney, Stephen L., O'Connor, Stephen J., Nelson, Lissa T.J., Sullivan, Gerard M., Imade, Hovis, Wang, Weibo, Hasvold, Lisa, Li, Qun, Cohen, Jerome, Gu, Wen-Zhen, Tahir, Stephen K., Bauch, Joy, Marsh, Kennan, Ng, Shi-Chung, Frost, David J., Zhang, Haiying, Muchmore, Steve, Jakob, Clarissa G., Stoll, Vincent, Hutchins, Charles, Rosenberg, Saul H., Sham, Hing L.
Published in Bioorganic & medicinal chemistry letters (07.04.2003)
Published in Bioorganic & medicinal chemistry letters (07.04.2003)
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Pyridone-Containing farnesyltransferase inhibitors: synthesis and biological evaluation
Hasvold, Lisa A., Wang, Weibo, Gwaltney, Stephen L., Rockway, Todd W., Nelson, Lissa T.J., Mantei, Robert A., Fakhoury, Stephen A., Sullivan, Gerard M., Li, Qun, Lin, Nan-Horng, Wang, Le, Zhang, Haiying, Cohen, Jerome, Gu, Wen-Zhen, Marsh, Kennan, Bauch, Joy, Rosenberg, Saul, Sham, Hing L.
Published in Bioorganic & medicinal chemistry letters (17.11.2003)
Published in Bioorganic & medicinal chemistry letters (17.11.2003)
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Preclinical Characterization of BET Family Bromodomain Inhibitor ABBV-075 Suggests Combination Therapeutic Strategies
Bui, Mai H, Lin, Xiaoyu, Albert, Daniel H, Li, Leiming, Lam, Lloyd T, Faivre, Emily J, Warder, Scott E, Huang, Xiaoli, Wilcox, Denise, Donawho, Cherrie K, Sheppard, George S, Wang, Le, Fidanze, Steve, Pratt, John K, Liu, Dachun, Hasvold, Lisa, Uziel, Tamar, Lu, Xin, Kohlhapp, Fred, Fang, Guowei, Elmore, Steven W, Rosenberg, Saul H, McDaniel, Keith F, Kati, Warren M, Shen, Yu
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Synthesis and Structure−Activity Relationships of 2-Pyridones: A Novel Series of Potent DNA Gyrase Inhibitors as Antibacterial Agents
Li, Qun, Chu, Daniel T. W, Claiborne, Akiyo, Cooper, Curt S, Lee, Cheuk M, Raye, Kathleen, Berst, Kristine B, Donner, Pamela, Wang, Weibo, Hasvold, Lisa, Fung, Anthony, Ma, Zhenkun, Tufano, Michael, Flamm, Robert, Shen, Linus L, Baranowski, John, Nilius, Angela, Alder, Jeff, Meulbroek, Jonathan, Marsh, Kennan, Crowell, DeAnne, Hui, Yuhua, Seif, Louis, Melcher, Laura M, Henry, Rodger, Spanton, Steven, Faghih, Ramin, Klein, Larry L, Tanaka, S. Ken, Plattner, Jacob J
Published in Journal of medicinal chemistry (02.08.1996)
Published in Journal of medicinal chemistry (02.08.1996)
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Structure-Guided Design of a Series of MCL‑1 Inhibitors with High Affinity and Selectivity
Bruncko, Milan, Wang, Le, Sheppard, George S, Phillips, Darren C, Tahir, Stephen K, Xue, John, Erickson, Scott, Fidanze, Steve, Fry, Elizabeth, Hasvold, Lisa, Jenkins, Gary J, Jin, Sha, Judge, Russell A, Kovar, Peter J, Madar, David, Nimmer, Paul, Park, Chang, Petros, Andrew M, Rosenberg, Saul H, Smith, Morey L, Song, Xiaohong, Sun, Chaohong, Tao, Zhi-Fu, Wang, Xilu, Xiao, Yu, Zhang, Haichao, Tse, Chris, Leverson, Joel D, Elmore, Steven W, Souers, Andrew J
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Discovery, SAR, synthesis, pharmacokinetic and biochemical characterization of A-192411: A novel fungicidal lipopeptide-(I)
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Published in Bioorganic & medicinal chemistry letters (10.02.2003)
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Discovery of a Potent and Selective BCL‑XL Inhibitor with in Vivo Activity
Tao, Zhi-Fu, Hasvold, Lisa, Wang, Le, Wang, Xilu, Petros, Andrew M, Park, Chang H, Boghaert, Erwin R, Catron, Nathaniel D, Chen, Jun, Colman, Peter M, Czabotar, Peter E, Deshayes, Kurt, Fairbrother, Wayne J, Flygare, John A, Hymowitz, Sarah G, Jin, Sha, Judge, Russell A, Koehler, Michael F. T, Kovar, Peter J, Lessene, Guillaume, Mitten, Michael J, Ndubaku, Chudi O, Nimmer, Paul, Purkey, Hans E, Oleksijew, Anatol, Phillips, Darren C, Sleebs, Brad E, Smith, Brian J, Smith, Morey L, Tahir, Stephen K, Watson, Keith G, Xiao, Yu, Xue, John, Zhang, Haichao, Zobel, Kerry, Rosenberg, Saul H, Tse, Chris, Leverson, Joel D, Elmore, Steven W, Souers, Andrew J
Published in ACS medicinal chemistry letters (09.10.2014)
Published in ACS medicinal chemistry letters (09.10.2014)
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