Search Results - "Eastman, Kyle J"

Applications of Fluorine in Medicinal Chemistry by Gillis, Eric P, Eastman, Kyle J, Hill, Matthew D, Donnelly, David J, Meanwell, Nicholas A

“…The role of fluorine in drug design and development is expanding rapidly as we learn more about the unique properties associated with this unusual element and…”
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Scalable Total Syntheses of N-Linked Tryptamine Dimers by Direct Indole−Aniline Coupling: Psychotrimine and Kapakahines B and F by Newhouse, Timothy, Lewis, Chad A, Eastman, Kyle J, Baran, Phil S

“…This report details the invention of a method to enable syntheses of psychotrimine (1) and the kapakahines F and B (2, 3) on a gram scale and in a minimum…”
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Regulated induced proximity targeting chimeras-RIPTACs-A heterobifunctional small molecule strategy for cancer selective therapies by Raina, Kanak, Forbes, Chris D, Stronk, Rebecca, Rappi, Jr, Jonathan P, Eastman, Kyle J, Zaware, Nilesh, Yu, Xinheng, Li, Hao, Bhardwaj, Amit, Gerritz, Samuel W, Forgione, Mia, Hundt, Abigail, King, Madeline P, Posner, Zoe M, Correia, Allison D, McGovern, Andrew, Puleo, David E, Chenard, Rebekka, Mousseau, James J, Vergara, J Ignacio, Garvin, Ethan, Macaluso, Jennifer, Martin, Michael, Bassoli, Kyle, Jones, Kelli, Garcia, Marco, Howard, Katia, Yaggi, Madeleine, Smith, Levi M, Chen, Jinshan M, Mayfield, Andrew B, De Leon, Cesar A, Hines, John, Kayser-Bricker, Katherine J, Crews, Craig M

“…We describe a protein proximity inducing therapeutic modality called Regulated Induced Proximity Targeting Chimeras or RIPTACs: heterobifunctional small…”
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Studies on the Mechanism of Action of Prekinamycin, a Member of the Diazoparaquinone Family of Natural Products:  Evidence for Both sp2 Radical and Orthoquinonemethide Intermediates by Feldman, Ken S, Eastman, Kyle J

“…The putative reductive activation chemistry of the diazoparaquinone antibiotics was modeled with Bu3Sn−H and prekinamycin dimethyl ether along with…”
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Ferrocene-based inhibitors of hepatitis C virus replication that target NS5A with low picomolar in vitro antiviral activity by Gadhachanda, Venkat R., Eastman, Kyle J., Wang, Qiuping, Phadke, Avinash S., Patel, Dharaben, Yang, Wengang, Marlor, Christopher W., Deshpande, Milind, Huang, Mingjun, Wiles, Jason A.

“…[Display omitted] •Exploited a metallocene to gain access to a biplanar pharmacophoric arrangement.•Leveraged this organometallic architecture in the design of…”
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Bioactivation of cyclopropyl rings by P450: an observation encountered during the optimisation of a series of hepatitis C virus NS5B inhibitors by Zhuo, Xiaoliang, Wang, Ying-Zi, Yeung, Kap-Sun, Zhu, Juliang, Huang, Xiaohua Stella, Parcella, Kyle E., Eastman, Kyle J., Kadow, John F., Meanwell, Nicholas A., Shu, Yue-Zhong, Johnson, Benjamin M.

“…1. Due to its unique C-C and C-H bonding properties, conformational preferences and relative hydrophilicity, the cyclopropyl ring has been used as a synthetic…”
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Phosphocholine conjugation: an unexpected in vivo conjugation pathway associated with hepatitis c ns5b inhibitors featuring a bicyclo[1.1.1]pentane by Zhuo, Xiaoliang, Cantone, Joseph L, Wang, Yingzi, Leet, John E, Drexler, Dieter M, Yeung, Kap-Sun, Huang, Xiaohua Stella, Eastman, Kyle J, Parcella, Kyle E, Mosure, Kathleen W, Soars, Matthew G, Kadow, John F, Johnson, Benjamin M

“…During a medicinal chemistry campaign to identify inhibitors of the hepatitis C virus nonstructural protein 5B (RNA-dependent RNA polymerase), a…”
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The discovery of a pan-genotypic, primer grip inhibitor of HCV NS5B polymerase by Eastman, Kyle J, Parcella, Kyle, Yeung, Kap-Sun, Grant-Young, Katharine A, Zhu, Juliang, Wang, Tao, Zhang, Zhongxing, Yin, Zhiwei, Beno, Brett R, Sheriff, Steven, Kish, Kevin, Tredup, Jeffrey, Jardel, Adam G, Halan, Vivek, Ghosh, Kaushik, Parker, Dawn, Mosure, Kathy, Fang, Hua, Wang, Ying-Kai, Lemm, Julie, Zhuo, Xiaoliang, Hanumegowda, Umesh, Rigat, Karen, Donoso, Maria, Tuttle, Maria, Zvyaga, Tatyana, Haarhoff, Zuzana, Meanwell, Nicholas A, Soars, Matthew G, Roberts, Susan B, Kadow, John F

“…The development of a series of novel 7-azabenzofurans exhibiting pan-genotype inhibition of HCV NS5B polymerase binding to the primer grip site is presented…”
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Identification of a novel series of potent HCV NS5B Site I inhibitors by Eastman, Kyle J, Yang, Zhong, Bender, John A, Mosure, Kathy, Lemm, Julie A, Meanwell, Nicholas A, Roberts, Susan B, Knipe, Jay, Kadow, John F

“…Efforts investigating spatially comparative alternates of the ethylene-bridged piperazine in BMS-791325 that would offer a maintained or improved virologic and…”
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A Proposal for the Mechanism-of-Action of Diazoparaquinone Natural Products by Feldman, Ken S, Eastman, Kyle J

“…Treatment of the representative diazoparaquinone prekinamycin dimethyl ether with Bu3SnH/AIBN in aromatic solvents furnishes moderate-to-good yields of formal…”
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Diazonamide Synthesis Studies:  Use of Negishi Coupling to Fashion Diazonamide-Related Biaryls with Defined Axial Chirality by Feldman, Ken S, Eastman, Kyle J, Lessene, Guillaume

“…The syntheses of a bis indole and an indole salicylate with the required axial chirality for diazonamide A are reported. Atropselectivity in these biaryl…”
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An oral androgen receptor RIPTAC for prostate cancer by Raina, Kanak, Eastman, Kyle J, Yu, Xinheng, Forbes, Chris D, Jones, Kelli M, Mousseau, James J, Li, Hao, Kayser-Bricker, Katherine J, Crews, Craig M

“…184 Background: Resistance to Androgen Receptor Signaling Inhibitors (ARSIs) in prostate cancer occurs in almost all patients and is driven primarily by…”
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Abstract 1629: Prostate cancer RIPTAC™ therapeutics demonstrate activity in preclinical models of Enzalutamide-resistant prostate cancer by Yu, Xinheng, Eastman, Kyle J., Raina, Kanak, Jones, Kelli M., Forbes, Chris D., Hundt, Abigail, Garcia, Marco, Stronk, Rebecca, Howard, Katia, McGovern, Andrew, Chenard, Rebekka, Denny, Allison, Forgione, Mia, Bassoli, Kyle, Garvin, Ethan, Mousseau, James J., Li, Hao, King, Madeline P., Bhardwaj, Amit, Kayser-Bricker, Katherine J., Crews, Craig M.

“…Abstract Background: Novel drugs are needed to tackle forms of prostate cancer that demonstrate resistance to hormonal agents. Halda has invented an innovative…”
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Studies on the Mechanism of Action of Prekinamycin, a Member of the Diazoparaquinone Family of Natural Products:  Evidence for Both sp 2 Radical and Orthoquinonemethide Intermediates by Feldman, Ken S., Eastman, Kyle J.

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Studies on the mechanism of action of prekinamycin, a member of the diazoparaquinone family of natural products : Evidence for both sp2radical and orthoquinonemethide intermediates by FELDMAN, Ken S, EASTMAN, Kyle J

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The discovery of a pan-genotypic, primer grip inhibitor of HCV NS5B polymeraseThe authors declare no competing interests.Electronic supplementary information (ESI) available. See DOI: 10.1039/c6md00636a by Eastman, Kyle J, Parcella, Kyle, Yeung, Kap-Sun, Grant-Young, Katharine A, Zhu, Juliang, Wang, Tao, Zhang, Zhongxing, Yin, Zhiwei, Beno, Brett R, Sheriff, Steven, Kish, Kevin, Tredup, Jeffrey, Jardel, Adam G, Halan, Vivek, Ghosh, Kaushik, Parker, Dawn, Mosure, Kathy, Fang, Hua, Wang, Ying-Kai, Lemm, Julie, Zhuo, Xiaoliang, Hanumegowda, Umesh, Rigat, Karen, Donoso, Maria, Tuttle, Maria, Zvyaga, Tatyana, Haarhoff, Zuzana, Meanwell, Nicholas A, Soars, Matthew G, Roberts, Susan B, Kadow, John F

“…The development of a series of novel 7-azabenzofurans exhibiting pan-genotype inhibition of HCV NS5B polymerase via binding to the primer grip site is…”
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The discovery of a pan-genotypic, primer grip inhibitor of HCV NS5B polymerase† †The authors declare no competing interests. ‡ ‡Electronic supplementary information (ESI) available. See DOI: 10.1039/c6md00636a by Eastman, Kyle J., Parcella, Kyle, Yeung, Kap-Sun, Grant-Young, Katharine A., Zhu, Juliang, Wang, Tao, Zhang, Zhongxing, Yin, Zhiwei, Beno, Brett R., Sheriff, Steven, Kish, Kevin, Tredup, Jeffrey, Jardel, Adam G., Halan, Vivek, Ghosh, Kaushik, Parker, Dawn, Mosure, Kathy, Fang, Hua, Wang, Ying-Kai, Lemm, Julie, Zhuo, Xiaoliang, Hanumegowda, Umesh, Rigat, Karen, Donoso, Maria, Tuttle, Maria, Zvyaga, Tatyana, Haarhoff, Zuzana, Meanwell, Nicholas A., Soars, Matthew G., Roberts, Susan B., Kadow, John F.

“…A series of novel 7-azabenzofurans exhibiting pan-genotype inhibition of HCV NS5B polymerase via binding to the primer grip site is presented. The development…”
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