Search Results - "Catherine R. Burton"

Discovery of new acylaminopyridines as GSK-3 inhibitors by a structure guided in-depth exploration of chemical space around a pyrrolopyridinone core by Sivaprakasam, Prasanna, Han, Xiaojun, Civiello, Rita L, Jacutin-Porte, Swanee, Kish, Kevin, Pokross, Matt, Lewis, Hal A, Ahmed, Nazia, Szapiel, Nicolas, Newitt, John A, Baldwin, Eric T, Xiao, Hong, Krause, Carol M, Park, Hyunsoo, Nophsker, Michelle, Lippy, Jonathan S, Burton, Catherine R, Langley, David R, Macor, John E, Dubowchik, Gene M

“…Glycogen synthase kinase-3 (GSK-3) has been proposed to play a crucial role in the pathogenesis of many diseases including cancer, stroke, bipolar disorders,…”
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Synthesis and Biological Evaluation of 1-Aryl-4,5-dihydro-1H-pyrazolo[3,4-d]pyrimidin-4-one Inhibitors of Cyclin-Dependent Kinases by Markwalder, Jay A, Arnone, Marc R, Benfield, Pamela A, Boisclair, Michael, Burton, Catherine R, Chang, Chong-Hwan, Cox, Sarah S, Czerniak, Philip M, Dean, Charity L, Doleniak, Deborah, Grafstrom, Robert, Harrison, Barbara A, Kaltenbach, Robert F, Nugiel, David A, Rossi, Karen A, Sherk, Susan R, Sisk, Lisa M, Stouten, Pieter, Trainor, George L, Worland, Peter, Seitz, Steven P

“…Using a high-throughput screening strategy, a series of 1-aryl-4,5-dihydro-1H-pyrazolo[3,4-d]pyrimidin-4-ones was identified that inhibit the cyclin-dependent…”
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Design, Structure–Activity Relationships, and In Vivo Evaluation of Potent and Brain-Penetrant Imidazo[1,2‑b]pyridazines as Glycogen Synthase Kinase-3β (GSK-3β) Inhibitors by Hartz, Richard A., Ahuja, Vijay T., Sivaprakasam, Prasanna, Xiao, Hong, Krause, Carol M., Clarke, Wendy J., Kish, Kevin, Lewis, Hal, Szapiel, Nicolas, Ravirala, Ramu, Mutalik, Sayali, Nakmode, Deepa, Shah, Devang, Burton, Catherine R., Macor, John E., Dubowchik, Gene M.

“…Glycogen synthase kinase-3 (GSK-3) is a serine/threonine kinase that regulates numerous cellular processes, including metabolism, proliferation, and cell…”
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Synthesis and Evaluation of Indenopyrazoles as Cyclin-Dependent Kinase Inhibitors. 2. Probing the Indeno Ring Substituent Pattern by Nugiel, David A, Vidwans, Anup, Etzkorn, Anna-Marie, Rossi, Karen A, Benfield, Pamela A, Burton, Catherine R, Cox, Sarah, Doleniak, Deborah, Seitz, Steven P

“…We disclose a novel series of indenopyrazole-based cyclin-dependent kinase (CDK) inhibitors. Kinetic experiments confirmed our initial molecular modeling…”
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Structure–activity relationship (SAR) studies on substituted N-(pyridin-3-yl)-2-amino-isonicotinamides as highly potent and selective glycogen synthase kinase-3 (GSK-3) inhibitors by Luo, Guanglin, Chen, Ling, Jacutin-Porte, Swanee, Han, Ying, Burton, Catherine R., Xiao, Hong, Krause, Carol M., Cao, Yang, Liu, Nengyin, Kish, Kevin, Lewis, Hal A., Macor, John E., Dubowchik, Gene M.

“…[Display omitted] In our continuing efforts to explore structure–activity relationships around the novel class of potent, isonicotinamide-based GSK3 inhibitors…”
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Discovery of 2‑(Anilino)pyrimidine-4-carboxamides as Highly Potent, Selective, and Orally Active Glycogen Synthase Kinase‑3 (GSK-3) Inhibitors by Hartz, Richard A., Ahuja, Vijay T., Luo, Guanglin, Chen, Ling, Sivaprakasam, Prasanna, Xiao, Hong, Krause, Carol M., Clarke, Wendy J., Xu, Songmei, Tokarski, John S., Kish, Kevin, Lewis, Hal, Szapiel, Nicolas, Ravirala, Ramu, Mutalik, Sayali, Nakmode, Deepa, Shah, Devang, Burton, Catherine R., Macor, John E., Dubowchik, Gene M.

“…Glycogen synthase kinase-3 (GSK-3) is a serine/threonine kinase that serves as an important regulator of a broad range of cellular functions. It has been…”
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Discovery of Isonicotinamides as Highly Selective, Brain Penetrable, and Orally Active Glycogen Synthase Kinase‑3 Inhibitors by Luo, Guanglin, Chen, Ling, Burton, Catherine R, Xiao, Hong, Sivaprakasam, Prasanna, Krause, Carol M, Cao, Yang, Liu, Nengyin, Lippy, Jonathan, Clarke, Wendy J, Snow, Kimberly, Raybon, Joseph, Arora, Vinod, Pokross, Matt, Kish, Kevin, Lewis, Hal A, Langley, David R, Macor, John E, Dubowchik, Gene M

“…GSK-3 is a serine/threonine kinase that has numerous substrates. Many of these proteins are involved in the regulation of diverse cellular functions, including…”
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Synthesis and Evaluation of Indenopyrazoles as Cyclin-Dependent Kinase Inhibitors. 3. Structure Activity Relationships at C3 by Yue, Eddy W, Higley, C. Anne, DiMeo, Susan V, Carini, David J, Nugiel, David A, Benware, Carrie, Benfield, Pamela A, Burton, Catherine R, Cox, Sarah, Grafstrom, Robert H, Sharp, Diane M, Sisk, Lisa M, Boylan, John F, Muckelbauer, Jodi K, Smallwood, Angela M, Chen, Haiying, Chang, Chong-Hwan, Seitz, Steven P, Trainor, George L

“…The identification of indeno[1,2-c]pyrazol-4-ones as inhibitors of cyclin-dependent kinases (CDKs) has led to the discovery of a series of novel and potent…”
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Acyl Guanidine Inhibitors of β‑Secretase (BACE-1): Optimization of a Micromolar Hit to a Nanomolar Lead via Iterative Solid- and Solution-Phase Library Synthesis by Gerritz, Samuel W, Zhai, Weixu, Shi, Shuhao, Zhu, Shirong, Toyn, Jeremy H, Meredith, Jere E, Iben, Lawrence G, Burton, Catherine R, Albright, Charles F, Good, Andrew C, Tebben, Andrew J, Muckelbauer, Jodi K, Camac, Daniel M, Metzler, William, Cook, Lynda S, Padmanabha, Ramesh, Lentz, Kimberley A, Sofia, Michael J, Poss, Michael A, Macor, John E, Thompson, Lorin A

“…This report describes the discovery and optimization of a BACE-1 inhibitor series containing an unusual acyl guanidine chemotype that was originally…”
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Discovery and Evaluation of BMS-708163, a Potent, Selective and Orally Bioavailable γ-Secretase Inhibitor by Gillman, Kevin W, Starrett, John E, Parker, Michael F, Xie, Kai, Bronson, Joanne J, Marcin, Lawrence R, McElhone, Kate E, Bergstrom, Carl P, Mate, Robert A, Williams, Richard, Meredith, Jere E, Burton, Catherine R, Barten, Donna M, Toyn, Jeremy H, Roberts, Susan B, Lentz, Kimberley A, Houston, John G, Zaczek, Robert, Albright, Charles F, Decicco, Carl P, Macor, John E, Olson, Richard E

“…During the course of our research efforts to develop a potent and selective γ-secretase inhibitor for the treatment of Alzheimer's disease, we investigated a…”
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Identification of selective inhibitors of cyclin dependent kinase 4 by Carini, David J, Kaltenbach, Robert F, Liu, Jie, Benfield, Pamela A, Boylan, John, Boisclair, Michael, Brizuela, Leonardo, Burton, Catherine R, Cox, Sarah, Grafstrom, Robert, Harrison, Barbara A, Harrison, Kimberly, Akamike, Emeka, Markwalder, Jay A, Nakano, Yuki, Seitz, Steven P, Sharp, Diane M, Trainor, George L, Sielecki, Thais M

“…A new structural type of kinase inhibitor, containing a benzocarbazole nucleus, has been identified. Members of the series are selective for inhibition of the…”
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Macrocyclic prolinyl acyl guanidines as inhibitors of β-secretase (BACE) by Boy, Kenneth M., Guernon, Jason M., Wu, Yong-Jin, Zhang, Yunhui, Shi, Joe, Zhai, Weixu, Zhu, Shirong, Gerritz, Samuel W., Toyn, Jeremy H., Meredith, Jere E., Barten, Donna M., Burton, Catherine R., Albright, Charles F., Good, Andrew C., Grace, James E., Lentz, Kimberley A., Olson, Richard E., Macor, John E., Thompson, Lorin A.

“…[Display omitted] The synthesis, evaluation, and structure–activity relationships of a class of acyl guanidines which inhibit the BACE-1 enzyme are presented…”
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Identification and Preclinical Evaluation of the Bicyclic Pyrimidine γ‑Secretase Modulator BMS-932481 by Boy, Kenneth M, Guernon, Jason M, Zuev, Dmitry S, Xu, Li, Zhang, Yunhui, Shi, Jianliang, Marcin, Lawrence R, Higgins, Mendi A, Wu, Yong-Jin, Krishnananthan, Subramaniam, Li, Jianqing, Trehan, Ashok, Smith, Daniel, Toyn, Jeremy H, Meredith, Jere E, Burton, Catherine R, Kimura, S. Roy, Zvyaga, Tatyana, Zhuo, Xiaoliang, Lentz, Kimberley A, Grace, James E, Denton, Rex, Morrison, John S, Mathur, Arvind, Albright, Charles F, Ahlijanian, Michael K, Olson, Richard E, Thompson, Lorin A, Macor, John E

“…A triazine hit identified from a screen of the BMS compound collection was optimized for potency, in vivo activity, and off-target profile to produce the…”
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The Amyloid-β Rise and γ-Secretase Inhibitor Potency Depend on the Level of Substrate Expression by Burton, Catherine R., Meredith, Jere E., Barten, Donna M., Goldstein, Margi E., Krause, Carol M., Kieras, Cathy J., Sisk, Lisa, Iben, Lawrence G., Polson, Craig, Thompson, Mark W., Lin, Xu-Alan, Corsa, Jason, Fiedler, Tracey, Pierdomenico, Maria, Cao, Yang, Roach, Arthur H., Cantone, Joseph L., Ford, Michael J., Drexler, Dieter M., Olson, Richard E., Yang, Michael G., Bergstrom, Carl P., McElhone, Kate E., Bronson, Joanne J., Macor, John E., Blat, Yuval, Grafstrom, Robert H., Stern, Andrew M., Seiffert, Dietmar A., Zaczek, Robert, Albright, Charles F., Toyn, Jeremy H.

“…The amyloid-β (Aβ) peptide, which likely plays a key role in Alzheimer disease, is derived from the amyloid-β precursor protein (APP) through consecutive…”
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Synthesis and SAR of indole-and 7-azaindole-1,3-dicarboxamide hydroxyethylamine inhibitors of BACE-1 by Marcin, Lawrence R., Higgins, Mendi A., Zusi, F. Christopher, Zhang, Yunhui, Dee, Michael F., Parker, Michael F., Muckelbauer, Jodi K., Camac, Daniel M., Morin, Paul E., Ramamurthy, Vidhyashankar, Tebben, Andrew J., Lentz, Kimberley A., Grace, James E., Marcinkeviciene, Jovita A., Kopcho, Lisa M., Burton, Catherine R., Barten, Donna M., Toyn, Jeremy H., Meredith, Jere E., Albright, Charles F., Bronson, Joanne J., Macor, John E., Thompson, Lorin A.

“…Indole- and 7-azaindole-1,3-dicarboxamide hydroxyethylamines exhibited potent and selective inhibition of BACE-1. An optimized analog (10n) demonstrated good…”
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Monosubstituted γ-lactam and conformationally constrained 1,3-diaminopropan-2-ol transition-state isostere inhibitors of β-secretase (BACE) by Boy, Kenneth M., Guernon, Jason M., Shi, Jianliang, Toyn, Jeremy H., Meredith, Jere E., Barten, Donna M., Burton, Catherine R., Albright, Charles F., Marcinkeviciene, Jovita, Good, Andrew C., Tebben, Andrew J., Muckelbauer, Jodi K., Camac, Daniel M., Lentz, Kimberley A., Bronson, Joanne J., Olson, Richard E., Macor, John E., Thompson, Lorin A.

“…The synthesis, evaluation, and structure–activity relationships of a class of γ-lactam 1,3-diaminopropan-2-ol transition-state isostere inhibitors of BACE are…”
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Synthesis and in vivo evaluation of cyclic diaminopropane BACE-1 inhibitors by Thompson, Lorin A., Shi, Jianliang, Decicco, Carl P., Tebben, Andrew J., Olson, Richard E., Boy, Kenneth M., Guernon, Jason M., Good, Andrew C., Liauw, Ann, Zheng, Changsheng, Copeland, Robert A., Combs, Andrew P., Trainor, George L., Camac, Daniel M., Muckelbauer, Jodi K., Lentz, Kimberley A., Grace, James E., Burton, Catherine R., Toyn, Jeremy H., Barten, Donna M., Marcinkeviciene, Jovita, Meredith, Jere E., Albright, Charles F., Macor, John E.

“…The synthesis, evaluation, and structure–activity relationships of a set of related constrained diaminopropane inhibitors of BACE-1 are described. The full in…”
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Synthesis and SAR of hydroxyethylamine based phenylcarboxyamides as inhibitors of BACE by Wu, Yong-Jin, Zhang, Yunhui, Good, Andrew C., Burton, Catherine R., Toyn, Jeremy H., Albright, Charles F., Macor, John E., Thompson, Lorin A.

“…A series of N-((2 S,3 R)-1-(3,5-difluorophenyl)-3-hydroxy-4-(3-methoxybenzylamino)-butan-2-yl)benzamides has been synthesized as BACE inhibitors. A variety of…”
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Indenopyrazoles as Novel Cyclin Dependent Kinase (CDK) Inhibitors by Nugiel, David A, Etzkorn, Ana-Marie, Vidwans, Anup, Benfield, Pamela A, Boisclair, Michael, Burton, Catherine R, Cox, Sarah, Czerniak, Phillip M, Doleniak, Deborah, Seitz, Steven P

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Quinazolines as cyclin dependent kinase inhibitors by Sielecki, Thais M., Johnson, Tricia L., Liu, Jie, Muckelbauer, Jodi K., Grafstrom, Robert H., Cox, Sarah, Boylan, John, Burton, Catherine R., Chen, Haiying, Smallwood, Angela, Chang, Chong-Hwan, Boisclair, Michael, Benfield, Pamela A., Trainor, George L., Seitz, Steven P.

“…Quinazolines have been identified as inhibitors of CDK4/D1 and CDK2/E. Aspects of the SAR were investigated using solution-phase, parallel synthesis. An X-ray…”
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