Search Results - "Hennessy, Edward"

Selective inhibitors of Bcl-2 and Bcl-xL: Balancing antitumor activity with on-target toxicity by Hennessy, Edward J.

“…[Display omitted] The induction of apoptosis in tumor cells represents a promising approach to the treatment of cancer. Accordingly, compounds that interact…”
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Synthesis of Substituted Oxindoles from α-Chloroacetanilides via Palladium-Catalyzed C−H Functionalization by Hennessy, Edward J, Buchwald, Stephen L

“…A novel method for the synthesis of oxindoles is described. In the presence of catalytic palladium acetate and 2-(di-tert-butylphosphino)biphenyl,…”
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Alternative Farnsworth-Munsell Scoring Methodology for Testing Eyewear by Hennessy, Edward R.

“…The Farnsworth-Munsell 100 Hue Test (FM100) has been used in clinical and ophthalmic settings for many years. It is a sensitive test for determining individual…”
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Discovery and Optimization of the First ATP Competitive Type-III c‑MET Inhibitor by Michaelides, Iacovos N., Collie, Gavin W., Börjesson, Ulf, Vasalou, Christina, Alkhatib, Omar, Barlind, Louise, Cheung, Tony, Dale, Ian L., Embrey, Kevin J., Hennessy, Edward J., Khurana, Puneet, Koh, Cheryl M., Lamb, Michelle L., Liu, Jianming, Moss, Thomas A., O’Neill, Daniel J., Phillips, Christopher, Shaw, Joseph, Snijder, Arjan, Storer, R. Ian, Stubbs, Christopher J., Han, Fujin, Li, Chengzhi, Qiao, Jingchuan, Sun, Dong-Qing, Wang, Jingwen, Wang, Peng, Yang, Wenzhen

“…Recent clinical reports have highlighted the need for wild-type (WT) and mutant dual inhibitors of c-MET kinase for the treatment of cancer. We report herein a…”
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Discovery of a Novel Class of Dimeric Smac Mimetics as Potent IAP Antagonists Resulting in a Clinical Candidate for the Treatment of Cancer (AZD5582) by Hennessy, Edward J, Adam, Ammar, Aquila, Brian M, Castriotta, Lillian M, Cook, Donald, Hattersley, Maureen, Hird, Alexander W, Huntington, Christopher, Kamhi, Victor M, Laing, Naomi M, Li, Danyang, MacIntyre, Terry, Omer, Charles A, Oza, Vibha, Patterson, Troy, Repik, Galina, Rooney, Michael T, Saeh, Jamal C, Sha, Li, Vasbinder, Melissa M, Wang, Haiyun, Whitston, David

“…A series of dimeric compounds based on the AVPI motif of Smac were designed and prepared as antagonists of the inhibitor of apoptosis proteins (IAPs)…”
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Optimization of an Imidazo[1,2‑a]pyridine Series to Afford Highly Selective Type I1/2 Dual Mer/Axl Kinase Inhibitors with In Vivo Efficacy by McCoull, William, Boyd, Scott, Brown, Martin R, Coen, Muireann, Collingwood, Olga, Davies, Nichola L, Doherty, Ann, Fairley, Gary, Goldberg, Kristin, Hardaker, Elizabeth, He, Guang, Hennessy, Edward J, Hopcroft, Philip, Hodgson, George, Jackson, Anne, Jiang, Xiefeng, Karmokar, Ankur, Lainé, Anne-Laure, Lindsay, Nicola, Mao, Yumeng, Markandu, Roshini, McMurray, Lindsay, McLean, Neville, Mooney, Lorraine, Musgrove, Helen, Nissink, J. Willem M, Pflug, Alexander, Reddy, Venkatesh Pilla, Rawlins, Philip B, Rivers, Emma, Schimpl, Marianne, Smith, Graham F, Tentarelli, Sharon, Travers, Jon, Troup, Robert I, Walton, Josephine, Wang, Cheng, Wilkinson, Stephen, Williamson, Beth, Winter-Holt, Jon, Yang, Dejian, Zheng, Yuting, Zhu, Qianxiu, Smith, Paul D

“…Inhibition of Mer and Axl kinases has been implicated as a potential way to improve the efficacy of current immuno-oncology therapeutics by restoring the…”
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Generating Selective Leads for Mer Kinase InhibitorsExample of a Comprehensive Lead-Generation Strategy by Nissink, J. Willem M, Bazzaz, Sana, Blackett, Carolyn, Clark, Matthew A, Collingwood, Olga, Disch, Jeremy S, Gikunju, Diana, Goldberg, Kristin, Guilinger, John P, Hardaker, Elizabeth, Hennessy, Edward J, Jetson, Rachael, Keefe, Anthony D, McCoull, William, McMurray, Lindsay, Olszewski, Allison, Overman, Ross, Pflug, Alexander, Preston, Marian, Rawlins, Philip B, Rivers, Emma, Schimpl, Marianne, Smith, Paul, Truman, Caroline, Underwood, Elizabeth, Warwicker, Juli, Winter-Holt, Jon, Woodcock, Simon, Zhang, Ying

“…Mer is a member of the TAM (Tyro3, Axl, Mer) kinase family that has been associated with cancer progression, metastasis, and drug resistance. Their essential…”
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Structural and Molecular Insight into Resistance Mechanisms of First Generation cMET Inhibitors by Collie, Gavin W, Koh, Cheryl M, O’Neill, Daniel J, Stubbs, Christopher J, Khurana, Puneet, Eddershaw, Alice, Snijder, Arjan, Mauritzson, Fredrik, Barlind, Louise, Dale, Ian L, Shaw, Joseph, Phillips, Christopher, Hennessy, Edward J, Cheung, Tony, Narvaez, Ana J

“…Many small molecule inhibitors of the cMET receptor tyrosine kinase have been evaluated in clinical trials for the treatment of cancer and…”
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Discovery of Potent KIFC1 Inhibitors Using a Method of Integrated High-Throughput Synthesis and Screening by Yang, Bin, Lamb, Michelle L, Zhang, Tao, Hennessy, Edward J, Grewal, Gurmit, Sha, Li, Zambrowski, Mark, Block, Michael H, Dowling, James E, Su, Nancy, Wu, Jiaquan, Deegan, Tracy, Mikule, Keith, Wang, Wenxian, Kaspera, Rüdiger, Chuaqui, Claudio, Chen, Huawei

“…KIFC1 (HSET), a member of the kinesin-14 family of motor proteins, plays an essential role in centrosomal bundling in cancer cells, but its function is not…”
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A General and Mild Copper-Catalyzed Arylation of Diethyl Malonate by Hennessy, Edward J, Buchwald, Stephen L

“…A general method for the synthesis of α-aryl malonates is described. The coupling of an aryl iodide and diethyl malonate in the presence of Cs2CO3 and…”
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Identification and Optimization of Benzimidazole Sulfonamides as Orally Bioavailable Sphingosine 1‑Phosphate Receptor 1 Antagonists with in Vivo Activity by Hennessy, Edward J., Oza, Vibha, Adam, Ammar, Byth, Kate, Castriotta, Lillian, Grewal, Gurmit, Hamilton, Geraldine A., Kamhi, Victor M., Lewis, Paula, Li, Danyang, Lyne, Paul, Öster, Linda, Rooney, Michael T., Saeh, Jamal C., Sha, Li, Su, Qibin, Wen, Shengua, Xue, Yafeng, Yang, Bin

“…We report here a novel series of benzimidazole sulfonamides that act as antagonists of the S1P1 receptor, identified by exploiting an understanding of the…”
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Small molecule inhibitor of apoptosis proteins antagonists: a patent review by Hird, Alexander W, Aquila, Brian M, Hennessy, Edward J, Vasbinder, Melissa M, Yang, Bin

“…The family of inhibitor of apoptosis proteins (IAPs) plays a key role in the suppression of proapoptotic signaling; hence, a small molecule that disrupts the…”
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Optimization of Highly Kinase Selective Bis-anilino Pyrimidine PAK1 Inhibitors by McCoull, William, Hennessy, Edward J, Blades, Kevin, Chuaqui, Claudio, Dowling, James E, Ferguson, Andrew D, Goldberg, Frederick W, Howe, Nicholas, Jones, Christopher R, Kemmitt, Paul D, Lamont, Gillian, Varnes, Jeffrey G, Ward, Richard A, Yang, Bin

“…Group I p21-activated kinase (PAK) inhibitors are indicated as important in cancer progression, but achieving high kinase selectivity has been challenging. A…”
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Discovery of heterocyclic sulfonamides as sphingosine 1-phosphate receptor 1 (S1P1) antagonists by Hennessy, Edward J., Grewal, Gurmit, Byth, Kate, Kamhi, Victor M., Li, Danyang, Lyne, Paul, Oza, Vibha, Ronco, Lucienne, Rooney, Michael T., Saeh, Jamal C., Su, Qibin

“…[Display omitted] We have discovered a novel class of heterocyclic sulfonamides that act as antagonists of the S1P1 receptor. While members of this series…”
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Discovery of aminopiperidine-based Smac mimetics as IAP antagonists by Hennessy, Edward J., Saeh, Jamal C., Sha, Li, MacIntyre, Terry, Wang, Haiyun, Larsen, Nicholas A., Aquila, Brian M., Ferguson, Andrew D., Laing, Naomi M., Omer, Charles A.

“…A series of structurally unique Smac mimetics that act as antagonists of inhibitor of apoptosis proteins (IAPs) has been discovered. While most previously…”
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Structure-based design and synthesis of tricyclic IAP (Inhibitors of Apoptosis Proteins) inhibitors by Hird, Alexander W., Aquila, Brian M., Block, Michael H., Hennessy, Edward J., Kamhi, Victor M., Omer, Charles A., Laing, Naomi M., Saeh, Jamal C., Sha, Li, Yang, Bin

“…The design and synthesis of a series of novel tricyclic IAP inhibitors is reported. Rapid assembly of the core tricycle involved two key steps: Rh-catalyzed…”
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Direct and selective elimination of specific prions and amyloids by 4,5-dianilinophthalimide and analogs by Wang, Huan, Duennwald, Martin L, Roberts, Blake E, Rozeboom, Leslie M, Zhang, Yingxin L, Steele, Andrew D, Krishnan, Rajaraman, Su, Linhui Julie, Griffin, Drees, Mukhopadhyay, Samrat, Hennessy, Edward J, Weigele, Peter, Blanchard, Barbara J, King, Jonathan, Deniz, Ashok A, Buchwald, Stephen L, Ingram, Vernon M, Lindquist, Susan, Shorter, James

“…Mechanisms to safely eliminate amyloids and preamyloid oligomers associated with many devastating diseases are urgently needed. Biophysical principles dictate…”
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Utilization of Structure-Based Design to Identify Novel, Irreversible Inhibitors of EGFR Harboring the T790M Mutation by Hennessy, Edward J, Chuaqui, Claudio, Ashton, Susan, Colclough, Nicola, Cross, Darren A. E, Debreczeni, Judit É, Eberlein, Cath, Gingipalli, Lakshmaiah, Klinowska, Teresa C. M, Orme, Jonathan P, Sha, Li, Wu, Xiaoyun

“…A novel series of covalent inhibitors of EGFR (epidermal growth factor receptor) kinase was discovered through a combination of subset screening and…”
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Preparation of highly functionalized 1,5-disubstituted tetrazoles via palladium-catalyzed Suzuki coupling by Hennessy, Edward J., Cornebise, Mark, Gingipalli, Lakshmaiah, Grebe, Tyler, Hande, Sudhir, Hoesch, Valerie, Huynh, Hoan, Throner, Scott, Varnes, Jeffrey, Wu, Ye

“…[Display omitted] •A variety of 1,5-disubstituted tetrazoles have been synthesized.•Substrates readily prepared from azides and p-toluenesulfonyl…”
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Evaluating the Effects of Clothing and Individual Equipment on Marksmanship Performance Using a Novel Five Target Methodology by McNamara, Jay A., Choi, Hyeg Joo, Brown, Stephanie A.T., Hennessy, Edward R., Mitchell, K. Blake

“…Any item of Warfighter-borne clothing and individual equipment (CIE) must not interfere with the Warfighter’s ability to quickly and accurately engage targets…”
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