Search Results - "LUKE, George P"

Discovery and Optimization of Quinolinone Derivatives as Potent, Selective, and Orally Bioavailable Mutant Isocitrate Dehydrogenase 1 (mIDH1) Inhibitors by Lin, Jian, Lu, Wei, Caravella, Justin A, Campbell, Ann Marie, Diebold, R. Bruce, Ericsson, Anna, Fritzen, Edward, Gustafson, Gary R, Lancia, David R, Shelekhin, Tatiana, Wang, Zhongguo, Castro, Jennifer, Clarke, Andrea, Gotur, Deepali, Josephine, Helen R, Katz, Marie, Diep, Hien, Kershaw, Mark, Yao, Lili, Kauffman, Goss, Hubbs, Stephen E, Luke, George P, Toms, Angela V, Wang, Liann, Bair, Kenneth W, Barr, Kenneth J, Dinsmore, Christopher, Walker, Duncan, Ashwell, Susan

“…Mutations at the arginine residue (R132) in isocitrate dehydrogenase 1 (IDH1) are frequently identified in various human cancers. Inhibition of mutant IDH1…”
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Discovery and optimization of novel piperazines as potent inhibitors of fatty acid synthase (FASN) by Martin, Matthew W., Lancia, David R., Li, Hongbin, Schiller, Shawn E.R., Toms, Angela V., Wang, Zhongguo, Bair, Kenneth W., Castro, Jennifer, Fessler, Shawn, Gotur, Deepali, Hubbs, Stephen E., Kauffman, Goss S., Kershaw, Mark, Luke, George P., McKinnon, Crystal, Yao, Lili, Lu, Wei, Millan, David S.

“…[Display omitted] •Identified novel and potent inhibitors of FASN KR domain.•Synthesis and structure activity relationships of compounds are reported.•FT113…”
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Design and Optimization of Benzopiperazines as Potent Inhibitors of BET Bromodomains by Millan, David S, Kayser-Bricker, Katherine J, Martin, Matthew W, Talbot, Adam C, Schiller, Shawn E. R, Herbertz, Torsten, Williams, Grace L, Luke, George P, Hubbs, Stephen, Alvarez Morales, Monica A, Cardillo, Daniel, Troccolo, Paul, Mendes, Rachel L, McKinnon, Crystal

“…A protein structure-guided drug design approach was employed to develop small molecule inhibitors of the BET family of bromodomains that were distinct from the…”
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Titanium and Boron Mediated Aldol Reactions of .beta.-Hydroxy Ketones by Luke, George P, Morris, Joel

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An Efficient Preparation of β-Aryl-β-ketophosphonates by the TFAA/H3PO4-Mediated Acylation of Arenes with Phosphonoacetic Acids by Luke, George P, Seekamp, Christopher K, Wang, Zhe-Qing, Chenard, Bertrand L

“…β-Aryl-β-ketophosphonates can be efficiently prepared in good yield by using a TFAA/85% H3PO4-mediated acylation of electron-rich arenes with phosphonoacetic…”
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Lewis Acid Promoted Additions of .gamma.-Alkoxy- and -(Silyloxy)crotylstannanes to (S)-2-(Benzyloxy)propanal by Marshall, James A, Jablonowski, Jill A, Luke, George P

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Formation of 1,3-diynes, 1,3-dienes, and biphenyls via the copper(II) nitrate mediated coupling of organotin compounds by Ghosal, Saswati, Luke, George P, Kyler, Keith S

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Bone-Targeted pyrido[2,3- d]pyrimidin-7-ones: potent inhibitors of Src tyrosine kinase as novel antiresorptive agents by Vu, Chi B., Luke, George P., Kawahata, Noriyuki, Shakespeare, William C., Wang, Yihan, Sundaramoorthi, Raji, Metcalf, Chester A., Keenan, Terence P., Pradeepan, Selvi, Corpuz, Evelyn, Merry, Taylor, Bohacek, Regine S., Dalgarno, David C., Narula, Surinder S., van Schravendijk, Marie Rose, Ram, Mary K., Adams, Susan, Liou, Shuenn, Keats, Jeffrey A., Violette, Shelia M., Guan, Wei, Weigele, Manfred, Sawyer, Tomi K.

“…The design of bone-targeted pyrido[2,3- d]pyrimidin-7-ones as Src tyrosine kinase inhibitors is described. Leveraging SAR from known compounds and using…”
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Structure-Based Design of Novel Bicyclic Nonpeptide Inhibitors for the Src SH2 Domain by Shakespeare, William C, Bohacek, Regine S, Azimioara, Mihai D, Macek, Karina J, Luke, George P, Dalgarno, David C, Hatada, Marcos H, Lu, Xiaode, Violette, Shelia M, Bartlett, Catherine, Sawyer, Tomi K

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Stereoselective total synthesis of bengamide E from glyceraldehyde acetonide and a nonracemic .gamma.-alkoxy allylic stannane by Marshall, James A, Luke, George P

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Reaction of Phosgeniminium Salts with Enolates Derived from Lewis Acid Complexes of 2‘-Hydroxypropiophenones and Related β-Diketones by Morris, Joel, Luke, George P, Wishka, Donn G

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Synthesis of ( S)-5-(1-aminoethyl)-2-(cyclohexylmethoxy)benzamide by Luke, George P, Holt, Dennis A

“…Three short syntheses of the title compound, a peptidomimetic for the Glu-Glu-Ile-NH 2 portion of Ac-pTyr-Glu-Glu-Ile-NH 2, a high affinity peptide for the Src…”
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Synthesis of Protected Carbohydrate Derivatives Through Homologation of Threose and Erythrose Derivatives with Chiral .gamma.-Alkoxy Allylic Stannanes by Marshall, James A, Seletsky, Boris M, Luke, George P

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A novel phosphotyrosine mimetic 4'-carboxymethyloxy-3'-phosphonophenylalanine (Cpp) : Exploitation in the design of nonpeptide inhibitors of pp60Src SH2 domain by KAWAHATA, Noriyuki, YANG, Michael G, BARTLETT, Catherine, SMITH, Jeremy, HATADA, Marcos, XIAODE LU, DALGARNO, David C, EYERMANN, Charles J, BOHACEK, Regine S, SAWYER, Tomi K, LUKE, George P, SHAKESPEARE, William C, SUNDARAMOORTHI, Raji, YIHAN WANG, JOHNSON, Daniel, MERRY, Taylor, VIOLETTE, Shelia, WEI GUAN

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FT-1101: A Structurally Distinct Pan-BET Bromodomain Inhibitor with Activity in Preclinical Models of Hematologic Malignancies by Millan, David S, Alvarez Morales, Monica A, Barr, Kenneth J, Cardillo, Daniel, Collis, Alan, Dinsmore, Christopher J, Escobedo, Jaime A, Foley, Kevin P, Herbertz, Torsten, Hubbs, Stephen, Kauffman, Goss S, Kayser-Bricker, Katherine J, Kershaw, Mark T, Luke, George P, Martin, Matthew W, McKinnon, Crystal, Mendes, Rachel L, Muskiewicz, Kristina R, Schiller, Shawn ER, Soulard, Patricia, Talbot, Adam C, Walker, Duncan, Yao, Lili, Williams, Grace L

“…Members of the Bromodomain and Extra-Terminal (BET) family of bromodomain-containing proteins (BRD2, BRD3, BRD4, and BRDT) bind to acetylated lysine residues…”
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Diastereoselective additions of enantioenriched .gamma.-(alkoxy)allyl stannanes to .alpha.-alkoxy aldehydes: a synthetic route to carbohydrates by Marshall, James A, Luke, George P

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An Efficient Preparation of β-Aryl-β-ketophosphonates by the TFAA/H 3 PO 4 -Mediated Acylation of Arenes with Phosphonoacetic Acids by Luke, George P., Seekamp, Christopher K., Wang, Zhe-Qing, Chenard, Bertrand L.

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A SIMPLE AND EFFICIENT PREPARATION OF (ARYLPHOSPHINYL)-METHYLPHOSPHONATES by Luke, George P., Shakespeare, William C.

“…A simple and efficient preparation of (arylphosphinyl)methylphosphonates is described whereby the phosphinylmethylphosphonate group is introduced via the Pd(0)…”
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Structure-based design and synthesis of a novel class of Src SH2 inhibitors by Buchanan, John L., Bohacek, Regine S., Luke, George P., Hatada, Marcos, Lu, Xiaode, Dalgarno, David C., Narula, Surinder S., Yuan, Ruth, Holt, Dennis A.

“…The structure-based design and synthesis of a novel class of 2,4-disubstituted thiazoles as Src SH2 inhibitors is described. Initial results are presented,…”
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A novel phosphotyrosine mimetic 4'-carboxymethyloxy-3'-phosphonophenylalanine (Cpp): exploitation in the design of nonpeptide inhibitors of pp60(Src) SH2 domain by Kawahata, N, Yang, M G, Luke, G P, Shakespeare, W C, Sundaramoorthi, R, Wang, Y, Johnson, D, Merry, T, Violette, S, Guan, W, Bartlett, C, Smith, J, Hatada, M, Lu, X, Dalgarno, D C, Eyermann, C J, Bohacek, R S, Sawyer, T K

“…The novel phosphotyrosine (pTyr) mimetic 4'-carboxymethyloxy-3'-phosphonophenylalanine (Cpp) has been designed and incorporated into a series of nonpeptide…”
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