Search Results - "BOSCHELLI, Diane H"

Discovery of Dibenzo[c,f][2,7]naphthyridines as Potent and Selective 3-Phosphoinositide-Dependent Kinase-1 Inhibitors by Gopalsamy, Ariamala, Shi, Mengxiao, Boschelli, Diane H, Williamson, Robert, Olland, Andrea, Hu, Yongbo, Krishnamurthy, Girija, Han, Xin, Arndt, Kim, Guo, Bing

“…With high-throughput screening, substituted dibenzo[c,f][2,7]naphthyridine 1 was identified as a novel potent and selective phosphoinositide-dependent kinase-1…”
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Neuroprotective profile of novel SRC kinase inhibitors in rodent models of cerebral ischemia by Liang, Shi, Pong, Kevin, Gonzales, Cathleen, Chen, Yi, Ling, Huai-Ping, Mark, Robert J, Boschelli, Frank, Boschelli, Diane H, Ye, Fei, Barrios Sosa, Ana Carolina, Mansour, Tarek S, Frost, Philip, Wood, Andrew, Pangalos, Menelas N, Zaleska, Margaret M

“…Src kinase signaling has been implicated in multiple mechanisms of ischemic injury, including vascular endothelial growth factor (VEGF)-mediated vascular…”
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Optimization of 4-Phenylamino-3-quinolinecarbonitriles as Potent Inhibitors of Src Kinase Activity by Boschelli, Diane H, Ye, Fei, Wang, Yanong D, Dutia, Minu, Johnson, Steve L, Wu, Biqi, Miller, Karen, Powell, Dennis W, Yaczko, Deanna, Young, Mairead, Tischler, Mark, Arndt, Kim, Discafani, Carolyn, Etienne, Carlo, Gibbons, Jay, Grod, Janet, Lucas, Judy, Weber, Jennifer M, Boschelli, Frank

“…Subsequent to the discovery of 4-[(2,4-dichlorophenyl)amino]-6,7-dimethoxy-3-quinolinecarbonitrile (1a) as an inhibitor of Src kinase activity (IC50 = 30 nM),…”
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Synthesis and Src Kinase Inhibitory Activity of a Series of 4-[(2,4-Dichloro-5-methoxyphenyl)amino]-7-furyl-3-quinolinecarbonitriles by Boschelli, Diane H, Wu, Biqi, Ye, Fei, Wang, Yan, Golas, Jennifer M, Lucas, Judy, Boschelli, Frank

“…Compound 1 (SKI-606, bosutinib), a 7-alkoxy-4-[(2,4-dichloro-5-methoxyphenyl)amino]-3-quinolinecarbonitrile, is a potent inhibitor of Src kinase activity. We…”
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Synthesis and Src Kinase Inhibitory Activity of a Series of 4-Phenylamino-3-quinolinecarbonitriles by Boschelli, Diane H, Wang, Yanong D, Ye, Fei, Wu, Biqi, Zhang, Nan, Dutia, Minu, Powell, Dennis W, Wissner, Allan, Arndt, Kim, Weber, Jennifer M, Boschelli, Frank

“…Screening of a directed compound library in a yeast-based assay identified 4-[(2,4-dichlorophenyl)amino]-6,7-dimethoxy-3-quinolinecarbonitrile (2a) as a Src…”
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2-Alkenylthieno[2,3- b]pyridine-5-carbonitriles: Potent and selective inhibitors of PKCθ by Nathan Tumey, L., Boschelli, Diane H., Lee, Julie, Chaudhary, Divya

“…A series of 2-alkenylamide thieno[2,3- b]pyridine inhibitors of PKCθ is described. SAR studies led to compound 8 which has excellent selectivity over a variety…”
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SKI-606, a 4-anilino-3-quinolinecarbonitrile dual inhibitor of Src and Abl kinases, is a potent antiproliferative agent against chronic myelogenous leukemia cells in culture and causes regression of K562 xenografts in nude mice by GOLAS, Jennifer M, ARNDT, Kim, ETIENNE, Carlo, LUCAS, Judy, NARDIN, Danielle, GIBBONS, James, FROST, Philip, FEI YE, BOSCHELLI, Diane H, BOSCHELLI, Frank

“…Constitutive tyrosine kinase activity of Bcr-Abl promotes proliferation and survival of chronic myelogenous leukemia (CML) cells. Inhibition of Bcr-Abl…”
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Identification and optimization of indolo[2,3-c]quinoline inhibitors of IRAK4 by Tumey, L. Nathan, Boschelli, Diane H., Bhagirath, Niala, Shim, Jaechul, Murphy, Elizabeth A., Goodwin, Deborah, Bennett, Eric M., Wang, Mengmeng, Lin, Lih-Ling, Press, Barry, Shen, Marina, Frisbie, Richard K., Morgan, Paul, Mohan, Shashi, Shin, Julia, Rao, Vikram R.

“…IRAK4 is responsible for initiating signaling from Toll-like receptors (TLRs) and members of the IL-1/18 receptor family. Kinase-inactive knock-ins and…”
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1,3,4-Oxadiazole, 1,3,4-thiadiazole, and 1,2,4-triazole analogs of the fenamates: in vitro inhibition of cyclooxygenase and 5-lipoxygenase activities by Boschelli, Diane H, Connor, David T, Bornemeier, Dirk A, Dyer, Richard D, Kennedy, John A, Kuipers, Paul J, Okonkwo, Godwin C, Schrier, Denis J, Wright, Clifford D

“…N-Arylanthranilic acids, known generically as the fenamates, are nonsteroidal antiinflammatory drugs (NSAIDs) that block the metabolism of arachidonic acid by…”
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SKI-606, a Src/Abl inhibitor with in vivo activity in colon tumor xenograft models by GALAS, Jennifer M, LUCAS, Judy, FANGBIAO LI, TITSCH, Craig, HUSELTON, Christine, CHAUDHARY, Inder, BOSCHELLI, Frank, ETIENNE, Carlo, GOLAS, Jonathan, DISCAFANI, Carolyn, SRIDHARAN, Latha, BOGHAERT, Erwin, ARNDT, Kim, FEI YE, BOSCHELLI, Diane H

“…Src up-regulation is a common event in human cancers. In colorectal cancer, increased Src levels are an indicator of poor prognosis, and progression to…”
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5-Vinyl-3-pyridinecarbonitrile inhibitors of PKCθ: Optimization of enzymatic and functional activity by Tumey, L. Nathan, Bhagirath, Niala, Brennan, Agnes, Brooijmans, Natasja, Lee, Julie, Yang, Xiaoke, Boschelli, Diane H.

“…We describe the optimization of enzymatic and cellular potency of a series of 5-vinyl-3-pyridinecarbonitrile inhibitors of PKCθ. PKCθ is a serine/threonine…”
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Exploitation of the 3-quinolinecarbonitrile template for SRC tyrosine kinase inhibitors by Boschelli, Diane H

“…In 2000, Wyeth reported that the 3-quinolinecarbonitrile ring system was a template for EGFR inhibitors. It soon became apparent that the group at C-4 of this…”
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Structure−Activity Relationships for 1-Phenylbenzimidazoles as Selective ATP Site Inhibitors of the Platelet-Derived Growth Factor Receptor by Palmer, Brian D, Smaill, Jeff B, Boyd, Maruta, Boschelli, Diane H, Doherty, Annette M, Hamby, James M, Khatana, Sonya S, Kramer, James B, Kraker, Alan J, Panek, Robert L, Lu, Gina H, Dahring, Tawny K, Winters, R. Thomas, Showalter, H. D. Hollis, Denny, William A

“…1-Phenylbenzimidazoles are shown to be a new class of ATP-site inhibitors of the platelet-derived growth factor receptor (PDGFR). Structure−activity…”
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First generation 5-vinyl-3-pyridinecarbonitrile PKCθ inhibitors by Niu, Chuansheng, Boschelli, Diane H., Tumey, L. Nathan, Bhagirath, Niala, Subrath, Joan, Shim, Jaechul, Wang, Yan, Wu, Biqi, Eid, Clark, Lee, Julie, Yang, Xiaoke, Brennan, Agnes, Chaudhary, Divya

“…The synthesis of a series of 5-vinyl-3-pyridinecarbonitriles resulted in a potent PKCθ inhibitor 23e, which had an IC 50 value of 4.7 nM for the inhibition of…”
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Lead identification to generate 3-cyanoquinoline inhibitors of insulin-like growth factor receptor (IGF-1R) for potential use in cancer treatment by Miller, Lori M., Mayer, Scott C., Berger, Dan M., Boschelli, Diane H., Boschelli, Frank, Di, Li, Du, Xuemei, Dutia, Minu, Floyd, Middleton B., Johnson, Mark, Kenny, Cynthia Hess, Krishnamurthy, Girija, Moy, Franklin, Petusky, Susan, Tkach, Diane, Torres, Nancy, Wu, Biqi, Xu, Weixin

“…The strategies, synthesis, and SAR behind novel cyanoquinoline IGFR inhibitors ( 1) are reported. Insulin-like growth factor receptor (IGF-1R) is a growth…”
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Optimization of 5-phenyl-3-pyridinecarbonitriles as PKCθ inhibitors by Boschelli, Diane H., Wang, Daniel, Prashad, Amar S., Subrath, Joan, Wu, Biqi, Niu, Chuan, Lee, Julie, Yang, Xiaoke, Brennan, Agnes, Chaudhary, Divya

“…Analog 13b with a 4-methylindol-5-ylamino group at C-4 and a 4-(2-(4-methylpiperazin-1-yl)ethoxy)phenyl group at C-5 had an IC 50 value of 7.4 nM for the…”
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7-alkoxy-4-phenylamino-3-quinolinecarbonitriles as dual inhibitors of Src and Abl kinases by BOSCHELLI, Diane H, WANG, Yanong D, JOHNSON, Steve, BIQI WU, FEI YE, BARRIOS SOSA, Ana Carolina, GOLAS, Jennifer M, BOSCHELLI, Frank

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Optimization of 7-alkene-3-quinolinecarbonitriles as Src kinase inhibitors by Boschelli, Diane H., Wang, Daniel, Wang, Yan, Wu, Biqi, Honores, Erick E., Barrios Sosa, Ana Carolina, Chaudhary, Inder, Golas, Jennifer, Lucas, Judy, Boschelli, Frank

“…The 7-alkene-3-quinolinecarbonitrile 20, a potent inhibitor of Src enzymatic and cellular activity with IC 50 values of 2.1 and 58 nM, respectively, had…”
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C-5 Substituted heteroaryl 3-pyridinecarbonitriles as PKCθ inhibitors: Part I by Subrath, Joan, Wang, Daniel, Wu, Biqi, Niu, Chuansheng, Boschelli, Diane H., Lee, Julie, Yang, Xiaoke, Brennan, Agnes, Chaudhary, Divya

“…Analog 6e with a 4-methylindol-5-ylamino group at C-4 and a 5-[(4-methylpiperazin-1-yl)methyl]-2-furyl group at C-5 had an IC 50 value of 4.5 nM for the…”
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Optimization of 5-vinylaryl-3-pyridinecarbonitriles as PKCθ inhibitors by Boschelli, Diane H., Subrath, Joan, Niu, Chuansheng, Wu, Biqi, Wang, Yan, Lee, Julie, Brennan, Agnes, Ho, Melisa, Deng, Bijia, Yang, Xiaoke, Xu, Xin, Leung, Louis, Wang, Jianyao, Atherton, James, Chaudhary, Divya

“…The 3-pyridinecarbonitrile 8 has an IC 50 value of 1.1 nM for the inhibition of PKCθ and blocks the production of IL-2 in both stimulated murine T cells (IC 50…”
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