Discovery of lirafugratinib (RLY-4008), a highly selective irreversible small-molecule inhibitor of FGFR2
Schönherr, Heike, Ayaz, Pelin, Taylor, Alexander M, Casaletto, Jessica B, Touré, B Barry, Moustakas, Demetri T, Hudson, Brandi M, Valverde, Roberto, Zhao, Songping, O'Hearn, Patrick J, Foster, Lindsey, Sharon, Dina A, Garfinkle, Sam, Giordanetto, Fabrizio, Lescarbeau, André, Kurukulasuriya, Ravi, Gerami-Moayed, Nastaran, Maglic, Dejan, Bruderek, Kamil, Naik, Gaauri, Gunaydin, Hakan, Mader, Mary M, Boezio, Alessandro A, McLean, Thomas H, Chen, Rongfeng, Wang, Yanxia, Shaw, David E, Watters, James, Bergstrom, Donald A
Published in Proceedings of the National Academy of Sciences - PNAS (06.02.2024)
Published in Proceedings of the National Academy of Sciences - PNAS (06.02.2024)
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Journal Article
Optimization of a Novel Quinazolinone-Based Series of Transient Receptor Potential A1 (TRPA1) Antagonists Demonstrating Potent in Vivo Activity
Schenkel, Laurie B, Olivieri, Philip R, Boezio, Alessandro A, Deak, Holly L, Emkey, Renee, Graceffa, Russell F, Gunaydin, Hakan, Guzman-Perez, Angel, Lee, Josie H, Teffera, Yohannes, Wang, Weiya, Youngblood, Beth D, Yu, Violeta L, Zhang, Maosheng, Gavva, Narender R, Lehto, Sonya G, Geuns-Meyer, Stephanie
Published in Journal of medicinal chemistry (24.03.2016)
Published in Journal of medicinal chemistry (24.03.2016)
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Journal Article
Structure-Based Design of Novel Class II c-Met Inhibitors: 2. SAR and Kinase Selectivity Profiles of the Pyrazolone Series
Liu, Longbin, Norman, Mark H, Lee, Matthew, Xi, Ning, Siegmund, Aaron, Boezio, Alessandro A, Booker, Shon, Choquette, Debbie, D’Angelo, Noel D, Germain, Julie, Yang, Kevin, Yang, Yajing, Zhang, Yihong, Bellon, Steven F, Whittington, Douglas A, Harmange, Jean-Christophe, Dominguez, Celia, Kim, Tae-Seong, Dussault, Isabelle
Published in Journal of medicinal chemistry (08.03.2012)
Published in Journal of medicinal chemistry (08.03.2012)
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Journal Article
Sulfonamides as Selective NaV1.7 Inhibitors: Optimizing Potency, Pharmacokinetics, and Metabolic Properties to Obtain Atropisomeric Quinolinone (AM-0466) that Affords Robust in Vivo Activity
Graceffa, Russell F, Boezio, Alessandro A, Able, Jessica, Altmann, Steven, Berry, Loren M, Boezio, Christiane, Butler, John R, Chu-Moyer, Margaret, Cooke, Melanie, DiMauro, Erin F, Dineen, Thomas A, Feric Bojic, Elma, Foti, Robert S, Fremeau, Robert T, Guzman-Perez, Angel, Gao, Hua, Gunaydin, Hakan, Huang, Hongbing, Huang, Liyue, Ilch, Christopher, Jarosh, Michael, Kornecook, Thomas, Kreiman, Charles R, La, Daniel S, Ligutti, Joseph, Milgram, Benjamin C, Lin, Min-Hwa Jasmine, Marx, Isaac E, Nguyen, Hanh N, Peterson, Emily A, Rescourio, Gwen, Roberts, John, Schenkel, Laurie, Shimanovich, Roman, Sparling, Brian A, Stellwagen, John, Taborn, Kristin, Vaida, Karina R, Wang, Jean, Yeoman, John, Yu, Violeta, Zhu, Dawn, Moyer, Bryan D, Weiss, Matthew M
Published in Journal of medicinal chemistry (27.07.2017)
Published in Journal of medicinal chemistry (27.07.2017)
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Journal Article
Discovery of (R)‑6-(1-(8-Fluoro-6-(1-methyl‑1H‑pyrazol-4-yl)-[1,2,4]triazolo[4,3‑a]pyridin-3-yl)ethyl)-3-(2-methoxyethoxy)-1,6-naphthyridin-5(6H)‑one (AMG 337), a Potent and Selective Inhibitor of MET with High Unbound Target Coverage and Robust In Vivo Antitumor Activity
Boezio, Alessandro A, Copeland, Katrina W, Rex, Karen, K. Albrecht, Brian, Bauer, David, Bellon, Steven F, Boezio, Christiane, Broome, Martin A, Choquette, Deborah, Coxon, Angela, Dussault, Isabelle, Hirai, Satoko, Lewis, Richard, Lin, Min-Hwa Jasmine, Lohman, Julia, Liu, Jingzhou, Peterson, Emily A, Potashman, Michele, Shimanovich, Roman, Teffera, Yohannes, Whittington, Douglas A, Vaida, Karina R, Harmange, Jean-Christophe
Published in Journal of medicinal chemistry (24.03.2016)
Published in Journal of medicinal chemistry (24.03.2016)
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Journal Article
The discovery of benzoxazine sulfonamide inhibitors of NaV1.7: Tools that bridge efficacy and target engagement
La, Daniel S., Peterson, Emily A., Bode, Christiane, Boezio, Alessandro A., Bregman, Howard, Chu-Moyer, Margaret Y., Coats, James, DiMauro, Erin F., Dineen, Thomas A., Du, Bingfan, Gao, Hua, Graceffa, Russell, Gunaydin, Hakan, Guzman-Perez, Angel, Fremeau, Robert, Huang, Xin, Ilch, Christopher, Kornecook, Thomas J., Kreiman, Charles, Ligutti, Joseph, Jasmine Lin, Min-Hwa, McDermott, Jeff S., Marx, Isaac, Matson, David J., McDonough, Stefan I., Moyer, Bryan D., Nho Nguyen, Hanh, Taborn, Kristin, Yu, Violeta, Weiss, Matthew M.
Published in Bioorganic & medicinal chemistry letters (01.08.2017)
Published in Bioorganic & medicinal chemistry letters (01.08.2017)
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Journal Article
1,2,4-Triazolsulfone: A novel isosteric replacement of acylsulfonamides in the context of NaV1.7 inhibition
Boezio, Alessandro A., Andrews, Kristin, Boezio, Christiane, Chu-Moyer, Margaret, Copeland, Katrina W., DiMauro, Erin F., Foti, Robert S., Fremeau, Robert T., Gao, Hua, Geuns-Meyer, Stephanie, Graceffa, Russell F., Gunaydin, Hakan, Huang, Hongbing, La, Daniel S., Ligutti, Joseph, Moyer, Bryan D., Peterson, Emily A., Yu, Violeta, Weiss, Matthew M.
Published in Bioorganic & medicinal chemistry letters (15.06.2018)
Published in Bioorganic & medicinal chemistry letters (15.06.2018)
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Journal Article
Discovery of Potent and Selective 8‑Fluorotriazolopyridine c‑Met Inhibitors
Peterson, Emily A, Teffera, Yohannes, Albrecht, Brian K, Bauer, David, Bellon, Steven F, Boezio, Alessandro, Boezio, Christiane, Broome, Martin A, Choquette, Deborah, Copeland, Katrina W, Dussault, Isabelle, Lewis, Richard, Lin, Min-Hwa Jasmine, Lohman, Julia, Liu, Jingzhou, Potashman, Michele, Rex, Karen, Shimanovich, Roman, Whittington, Douglas A, Vaida, Karina R, Harmange, Jean-Christophe
Published in Journal of medicinal chemistry (12.03.2015)
Published in Journal of medicinal chemistry (12.03.2015)
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Journal Article
Pharmacological effects of nonselective and subtype-selective nicotinic acetylcholine receptor agonists in animal models of persistent pain
Gao, BaoXi, Hierl, Markus, Clarkin, Kristie, Juan, Todd, Nguyen, Hung, Valk, Marissa van der, Deng, Hong, Guo, Wenhong, Lehto, Sonya G., Matson, David, McDermott, Jeff S., Knop, Johannes, Gaida, Kevin, Cao, Lei, Waldon, Dan, Albrecht, Brian K., Boezio, Alessandro A., Copeland, Katrina W., Harmange, Jean-Christophe, Springer, Stephanie K., Malmberg, Annika B., McDonough, Stefan I.
Published in Pain (Amsterdam) (01.04.2010)
Published in Pain (Amsterdam) (01.04.2010)
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Journal Article
Development of novel azabenzofuran TRPA1 antagonists as in vivo tools
Copeland, Katrina W., Boezio, Alessandro A., Cheung, Eugene, Lee, Josie, Olivieri, Philip, Schenkel, Laurie B., Wan, Qian, Wang, Weiya, Wells, Mary C., Youngblood, Beth, Gavva, Narender R., Lehto, Sonya G., Geuns-Meyer, Stephanie
Published in Bioorganic & medicinal chemistry letters (01.08.2014)
Published in Bioorganic & medicinal chemistry letters (01.08.2014)
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Journal Article
1,2,4-Triazolsulfone: A novel isosteric replacement of acylsulfonamides in the context of Na V 1.7 inhibition
Boezio, Alessandro A, Andrews, Kristin, Boezio, Christiane, Chu-Moyer, Margaret, Copeland, Katrina W, DiMauro, Erin F, Foti, Robert S, Fremeau, Jr, Robert T, Gao, Hua, Geuns-Meyer, Stephanie, Graceffa, Russell F, Gunaydin, Hakan, Huang, Hongbing, La, Daniel S, Ligutti, Joseph, Moyer, Bryan D, Peterson, Emily A, Yu, Violeta, Weiss, Matthew M
Published in Bioorganic & medicinal chemistry letters (15.06.2018)
Published in Bioorganic & medicinal chemistry letters (15.06.2018)
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Journal Article
Sulfonamides as Selective Na V 1.7 Inhibitors: Optimizing Potency, Pharmacokinetics, and Metabolic Properties to Obtain Atropisomeric Quinolinone (AM-0466) that Affords Robust in Vivo Activity
Graceffa, Russell F, Boezio, Alessandro A, Able, Jessica, Altmann, Steven, Berry, Loren M, Boezio, Christiane, Butler, John R, Chu-Moyer, Margaret, Cooke, Melanie, DiMauro, Erin F, Dineen, Thomas A, Feric Bojic, Elma, Foti, Robert S, Fremeau, Jr, Robert T, Guzman-Perez, Angel, Gao, Hua, Gunaydin, Hakan, Huang, Hongbing, Huang, Liyue, Ilch, Christopher, Jarosh, Michael, Kornecook, Thomas, Kreiman, Charles R, La, Daniel S, Ligutti, Joseph, Milgram, Benjamin C, Lin, Min-Hwa Jasmine, Marx, Isaac E, Nguyen, Hanh N, Peterson, Emily A, Rescourio, Gwen, Roberts, John, Schenkel, Laurie, Shimanovich, Roman, Sparling, Brian A, Stellwagen, John, Taborn, Kristin, Vaida, Karina R, Wang, Jean, Yeoman, John, Yu, Violeta, Zhu, Dawn, Moyer, Bryan D, Weiss, Matthew M
Published in Journal of medicinal chemistry (27.07.2017)
Published in Journal of medicinal chemistry (27.07.2017)
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Journal Article
The discovery of benzoxazine sulfonamide inhibitors of Na V 1.7: Tools that bridge efficacy and target engagement
La, Daniel S, Peterson, Emily A, Bode, Christiane, Boezio, Alessandro A, Bregman, Howard, Chu-Moyer, Margaret Y, Coats, James, DiMauro, Erin F, Dineen, Thomas A, Du, Bingfan, Gao, Hua, Graceffa, Russell, Gunaydin, Hakan, Guzman-Perez, Angel, Fremeau, Jr, Robert, Huang, Xin, Ilch, Christopher, Kornecook, Thomas J, Kreiman, Charles, Ligutti, Joseph, Jasmine Lin, Min-Hwa, McDermott, Jeff S, Marx, Isaac, Matson, David J, McDonough, Stefan I, Moyer, Bryan D, Nho Nguyen, Hanh, Taborn, Kristin, Yu, Violeta, Weiss, Matthew M
Published in Bioorganic & medicinal chemistry letters (01.08.2017)
Published in Bioorganic & medicinal chemistry letters (01.08.2017)
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Journal Article
Efficient Total Syntheses of (−)-Colombiasin A and (−)-Elisapterosin B: Application of the Cr-Catalyzed Asymmetric Quinone Diels-Alder Reaction
Boezio, Alessandro A., Jarvo, Elizabeth R., Lawrence, Brian M., Jacobsen, Eric N.
Published in Angewandte Chemie International Edition (19.09.2005)
Published in Angewandte Chemie International Edition (19.09.2005)
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