Search Results - "Lucas, Brian S"

Total Synthesis of Phorboxazole B by Lucas, Brian S., Gopalsamuthiram, Vijayagopal, Burke, Steven D.

“…Challenge met: In the synthesis of phorboxazole B, a highly efficient hetero‐Diels–Alder reaction was used to construct the key C33–C39 linchpin, allowing for…”
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Synthesis of the C1−C17 Segment of Phorboxazole B by Lucas, Brian S, Luther, Laura M, Burke, Steven D

“…The C1−C17 bis-oxane subunit 22 of phorboxazole B is efficiently synthesized by exploiting differential reactivities between similar substituents on the…”
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An Expeditious Synthesis of the MDM2–p53 Inhibitor AM-8553 by Lucas, Brian S, Fisher, Benjamin, McGee, Lawrence R, Olson, Steven H, Medina, Julio C, Cheung, Eugene

“…The development of the structurally complex MDM2/p53 inhibitor AM-8553 was impeded by the low yield of the initial synthesis. A second generation synthesis is…”
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Discovery and in Vivo Evaluation of the Potent and Selective PI3Kδ Inhibitors 2‑((1S)‑1-((6-Amino-5-cyano-4-pyrimidinyl)amino)ethyl)-6-fluoro‑N‑methyl-3-(2-pyridinyl)-4-quinolinecarboxamide (AM-0687) and 2‑((1S)‑1-((6-Amino-5-cyano-4-pyrimidinyl)amino)ethyl)-5-fluoro‑N‑methyl-3-(2-pyridinyl)-4-quinolinecarboxamide (AM-1430) by Gonzalez-Lopez de Turiso, Felix, Hao, Xiaolin, Shin, Youngsook, Bui, Minna, Campuzano, Iain D. G, Cardozo, Mario, Dunn, Michelle C, Duquette, Jason, Fisher, Benjamin, Foti, Robert S, Henne, Kirk, He, Xiao, Hu, Yi-Ling, Kelly, Ron C, Johnson, Michael G, Lucas, Brian S, McCarter, John, McGee, Lawrence R, Medina, Julio C, Metz, Daniela, San Miguel, Tisha, Mohn, Deanna, Tran, Thuy, Vissinga, Christine, Wannberg, Sharon, Whittington, Douglas A, Whoriskey, John, Yu, Gang, Zalameda, Leeanne, Zhang, Xuxia, Cushing, Timothy D

“…Optimization of the potency and pharmacokinetic profile of 2,3,4-trisubstituted quinoline, 4, led to the discovery of two potent, selective, and orally…”
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Addressing PXR liabilities of phthalazine-based hedgehog/smoothened antagonists using novel pyridopyridazines by Kaizerman, Jacob A., Aaron, Wade, An, Songzhu, Austin, Richard, Brown, Matt, Chong, Angela, Huang, Tom, Hungate, Randall, Jiang, Ben, Johnson, Michael G., Lee, Gary, Lucas, Brian S., Orf, Jessica, Rong, Minqing, Toteva, Maria M., Wickramasinghe, Dineli, Xu, Guifen, Ye, Qiuping, Zhong, Wendy, McMinn, Dustin L.

“…Pyridopyridazine antagonists of the hedgehog signaling pathway are described. Designed to optimize our previously described phthalazine smoothened antagonists,…”
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Discovery of amide replacements that improve activity and metabolic stability of a bis-amide smoothened antagonist hit by Brown, Matthew L., Aaron, Wade, Austin, Richard J., Chong, Angela, Huang, Tom, Jiang, Ben, Kaizerman, Jacob A., Lee, Gary, Lucas, Brian S., McMinn, Dustin L., Orf, Jessica, Rong, Minqing, Toteva, Maria M., Xu, Guifen, Ye, Qiuping, Zhong, Wendy, DeGraffenreid, Michael R., Wickramasinghe, Dineli, Powers, Jay P., Hungate, Randall, Johnson, Michael G.

“…A bis-amide antagonist of Smoothened, a seven-transmembrane receptor in the Hedgehog signaling pathway, was discovered via high throughput screening. In vitro…”
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Palladium(0)-Mediated Desymmetrization of Meso Tetraols:  An Approach to the C3−C17 Bis-oxane Segment of Phorboxazoles A and B by Lucas, Brian S, Burke, Steven D

“…meso-Tetraol bis(allylic acetates) 2 and 5 were synthesized via two-directional chain elongation. A palladium-mediated, ligand-controlled desymmetrization…”
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Design of 1-piperazinyl-4-arylphthalazines as potent Smoothened antagonists by Lucas, Brian S., Aaron, Wade, An, Songzhu, Austin, Richard J., Brown, Matthew, Chan, Hon, Chong, Angela, Hungate, Randall, Huang, Tom, Jiang, Ben, Johnson, Michael G., Kaizerman, Jacob A., Lee, Gary, McMinn, Dustin L., Orf, Jessica, Powers, Jay P., Rong, Minqing, Toteva, Maria M., Uyeda, Craig, Wickramasinghe, Dineli, Xu, Guifen, Ye, Qiuping, Zhong, Wendy

“…The Hedgehog (Hh) signaling pathway regulates cell proliferation and differentiation in developing tissues, and abnormal activation of the Hh pathway has been…”
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A Catalytic Enantioselective Hetero Diels−Alder Approach to the C20−C32 Segment of the Phorboxazoles by Lucas, Brian S, Luther, Laura M, Burke, Steven D

“…An efficient synthesis of the C20−C32 segment of the phorboxazoles has been achieved using an enantioselective hetero Diels−Alder reaction catalyzed by…”
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Development of an Efficient Process for the Preparation of Sch 39166:  Aziridinium Chemistry on Scale by Gala, Dinesh, Dahanukar, Vilas H, Eckert, Jeffery M, Lucas, Brian S, Schumacher, Doris P, Zavialov, Ilia A, Buholzer, Patrik, Kubisch, Peter, Mergelsberg, Ingrid, Scherer, Dominik

“…A large-scale synthesis of a tricyclic D1/D5 dopamine antagonist based on regio- and stereoselective ring opening of an aziridinium ion with a Grignard reagent…”
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Reaction of aziridinium ions with organometallic reagents: optimization of the key step of ecopipam synthesis by Andrews, David R, Dahanukar, Vilas H, Eckert, Jeffrey M, Gala, Dinesh, Lucas, Brian S, Schumacher, Doris P, Zavialov, Ilia A

“…Formation, stability and reactivity of aziridinium ions 3 towards organometallic reagents was explored and optimized for the efficient preparation of key drug…”
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Anaesthesia in a parturient with Noonan's syndrome by GRANGE, C. S, HEID, R, LUCAS, S. B, ROSS, P. L. E, DOUGLAS, M. J

“…To report the management of labour analgesia and subsequent anaesthesia for postpartum bleeding in a 19-yr-old parturient with Noonan's syndrome. The patient…”
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Total Synthesis of Phorboxazole B by Lucas, Brian S., Gopalsamuthiram, Vijayagopal, Burke, Steven D.

“…Ziel erreicht: Bei der Synthese von Phorboxazol B wurde mit einer hocheffizienten Hetero‐Diels‐Alder‐Reaktion das zentrale C33‐C39‐Schlüsselelement erhalten,…”
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Total Synthesis of Phorboxazole B by Lucas, Brian S., Gopalsamuthiram, Vijayagopal, Burke, Steven D.

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Anaesthetic management and non-invasive monitoring for caesarean section in a patient with cardiomyopathy by GAMBLING, D. R, FLANAGAN, M. L, HUCKELL, V. F, LUCAS, S. B, KIM, J. H. K

“…This paper describes the anaesthetic management of a 29-year-old woman for an elective repeat Caesarean section. A diagnosis of peripartum cardiomyopathy…”
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