DNA-Encoded Library Technology-Based Discovery, Lead Optimization, and Prodrug Strategy toward Structurally Unique Indoleamine 2,3-Dioxygenase-1 (IDO1) Inhibitors
Kazmierski, Wieslaw M, Xia, Bing, Miller, John, De la Rosa, Martha, Favre, David, Dunham, Richard M, Washio, Yoshiaki, Zhu, Zhengrong, Wang, Feng, Mebrahtu, Makda, Deng, Hongfeng, Basilla, Jonathan, Wang, Liping, Evindar, Ghotas, Fan, Lijun, Olszewski, Alison, Prabhu, Ninad, Davie, Christopher, Messer, Jeffrey A, Samano, Vicente
Published in Journal of medicinal chemistry (09.04.2020)
Published in Journal of medicinal chemistry (09.04.2020)
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Journal Article
GSK2818713, a Novel Biphenylene Scaffold-Based Hepatitis C NS5A Replication Complex Inhibitor with Broad Genotype Coverage
Kazmierski, Wieslaw M, Baskaran, Sam, Walker, Jill T, Miriyala, Nagaraju, Meesala, Ramu, Beesu, Mallesh, Adjabeng, George, Grimes, Richard M, Hamatake, Robert, Leivers, Martin R, Crosby, Renae, Xia, Bing, Remlinger, Katja
Published in Journal of medicinal chemistry (23.04.2020)
Published in Journal of medicinal chemistry (23.04.2020)
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Journal Article
Novel Spiroketal Pyrrolidine GSK2336805 Potently Inhibits Key Hepatitis C Virus Genotype 1b Mutants: From Lead to Clinical Compound
Kazmierski, Wieslaw M., Maynard, Andrew, Duan, Maosheng, Baskaran, Sam, Botyanszki, Janos, Crosby, Renae, Dickerson, Scott, Tallant, Matthew, Grimes, Rick, Hamatake, Robert, Leivers, Martin, Roberts, Christopher D., Walker, Jill
Published in Journal of medicinal chemistry (13.03.2014)
Published in Journal of medicinal chemistry (13.03.2014)
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Journal Article
Preclinical Characterization of GSK2336805, a Novel Inhibitor of Hepatitis C Virus Replication That Selects for Resistance in NS5A
WALKER, Jill, CROSBY, Renae, HAMATAKE, Robert, AMY WANG, WOLDU, Ermias, VAMATHEVAN, Jessica, VOITENLEITNER, Christian, SHIHYUN YOU, REMLINGER, Katja, MAOSHANG DUAN, KAZMIERSKI, Wieslaw
Published in Antimicrobial Agents and Chemotherapy (01.01.2014)
Published in Antimicrobial Agents and Chemotherapy (01.01.2014)
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The relative activity of "function sparing" HIV-1 entry inhibitors on viral entry and CCR5 internalization: is allosteric functional selectivity a valuable therapeutic property?
Muniz-Medina, Vanessa M, Jones, Stacey, Maglich, Jodi M, Galardi, Cristin, Hollingsworth, Robert E, Kazmierski, Wieslaw M, Ferris, Robert G, Edelstein, Mark P, Chiswell, Karen E, Kenakin, Terry P
Published in Molecular pharmacology (01.03.2009)
Published in Molecular pharmacology (01.03.2009)
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Journal Article
Discovery of Novel Urea-Based Hepatitis C Protease Inhibitors with High Potency against Protease-Inhibitor-Resistant Mutants
Kazmierski, Wieslaw M, Hamatake, Robert, Duan, Maosheng, Wright, Lois L, Smith, Gary K, Jarvest, Richard L, Ji, Jing-Jing, Cooper, Joel P, Tallant, Matthew D, Crosby, Renae M, Creech, Katrina, Wang, Amy, Li, Xianfeng, Zhang, Suoming, Zhang, Yong-Kang, Liu, Yang, Ding, Charles Z, Zhou, Yasheen, Plattner, Jacob J, Baker, Stephen J, Bu, Wei, Liu, Liang
Published in Journal of medicinal chemistry (12.04.2012)
Published in Journal of medicinal chemistry (12.04.2012)
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Journal Article
Biological and Structural Characterization of Rotamers of C–C Chemokine Receptor Type 5 (CCR5) Inhibitor GSK214096
Kazmierski, Wieslaw M, Danehower, Susan, Duan, Maosheng, Ferris, Robert G, Elitzin, Vassil, Minick, Douglas, Sharp, Matthew, Stewart, Eugene, Villeneuve, Manon
Published in ACS medicinal chemistry letters (11.12.2014)
Published in ACS medicinal chemistry letters (11.12.2014)
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Journal Article
Novel 4,4-Disubstituted Piperidine-Based C–C Chemokine Receptor-5 Inhibitors with High Potency against Human Immunodeficiency Virus-1 and an Improved human Ether-a-go-go Related Gene (hERG) Profile
Kazmierski, Wieslaw M, Anderson, Don L, Aquino, Christopher, Chauder, Brian A, Duan, Maosheng, Ferris, Robert, Kenakin, Terrence, Koble, Cecilia S, Lang, Dan G, Mcintyre, Maggie S, Peckham, Jennifer, Watson, Christian, Wheelan, Pat, Spaltenstein, Andrew, Wire, Mary B, Svolto, Angilique, Youngman, Michael
Published in Journal of medicinal chemistry (09.06.2011)
Published in Journal of medicinal chemistry (09.06.2011)
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Journal Article
Discovery of a novel series of cyclic urea as potent CCR5 antagonists
Duan, Maosheng, Kazmierski, Wieslaw M., Tallant, Matt, Jun, Jung Ho, Edelstein, Mark, Ferris, Rob, Todd, Dan, Wheelan, Pat, Xiong, Zhiping
Published in Bioorganic & medicinal chemistry letters (01.11.2011)
Published in Bioorganic & medicinal chemistry letters (01.11.2011)
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Journal Article
Synthesis and biological evaluations of P4-benzoxaborole-substituted macrocyclic inhibitors of HCV NS3 protease
Ding, Charles Z., Zhang, Yong-Kang, Li, Xianfeng, Liu, Yang, Zhang, Suoming, Zhou, Yasheen, Plattner, Jacob J., Baker, Stephen J., Liu, Liang, Duan, Maosheng, Jarvest, Richard L., Ji, Jingjing, Kazmierski, Wieslaw M., Tallant, Matthew D., Wright, Lois L., Smith, Gary K., Crosby, Renae M., Wang, Amy A., Ni, Zhi-Jie, Zou, Wuxin, Wright, Jon
Published in Bioorganic & medicinal chemistry letters (15.12.2010)
Published in Bioorganic & medicinal chemistry letters (15.12.2010)
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Journal Article
Synthesis and SAR of acyclic HCV NS3 protease inhibitors with novel P4-benzoxaborole moieties
Li, Xianfeng, Zhang, Suoming, Zhang, Yong-Kang, Liu, Yang, Ding, Charles Z., Zhou, Yasheen, Plattner, Jacob J., Baker, Stephen J., Bu, Wei, Liu, Liang, Kazmierski, Wieslaw M., Duan, Maosheng, Grimes, Richard M., Wright, Lois L., Smith, Gary K., Jarvest, Richard L., Ji, Jing-Jing, Cooper, Joel P., Tallant, Matthew D., Crosby, Renae M., Creech, Katrina, Ni, Zhi-Jie, Zou, Wuxin, Wright, Jon
Published in Bioorganic & medicinal chemistry letters (01.04.2011)
Published in Bioorganic & medicinal chemistry letters (01.04.2011)
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Journal Article
Discovery of next generation inhibitors of HIV protease
Spaltenstein, Andrew, Kazmierski, Wieslaw M, Miller, John F, Samano, Vicente
Published in Current topics in medicinal chemistry (01.12.2005)
Published in Current topics in medicinal chemistry (01.12.2005)
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Journal Article
Synthesis and evaluation of novel α-amino cyclic boronates as inhibitors of HCV NS3 protease
Li, Xianfeng, Zhang, Yong-Kang, Liu, Yang, Ding, Charles Z., Li, Qun, Zhou, Yasheen, Plattner, Jacob J., Baker, Stephen J., Qian, Xuelei, Fan, Dazhong, Liao, Liang, Ni, Zhi-Jie, White, Gemma V., Mordaunt, Jackie E., Lazarides, Linos X., Slater, Martin J., Jarvest, Richard L., Thommes, Pia, Ellis, Malcolm, Edge, Colin M., Hubbard, Julia A., Somers, Don, Rowland, Paul, Nassau, Pamela, McDowell, Bill, Skarzynski, Tadeusz J., Kazmierski, Wieslaw M., Grimes, Richard M., Wright, Lois L., Smith, Gary K., Zou, Wuxin, Wright, Jon, Pennicott, Lewis E.
Published in Bioorganic & medicinal chemistry letters (15.06.2010)
Published in Bioorganic & medicinal chemistry letters (15.06.2010)
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Journal Article
Discovery of N-benzyl- N′-(4-pipyridinyl)urea CCR5 antagonists as anti-HIV-1 agents (I): Optimization of the amine portion
Duan, Maosheng, Peckham, Jennifer, Edelstein, Mark, Ferris, Robert, Kazmierski, Wieslaw M., Spaltenstein, Andrew, Wheelan, Pat, Xiong, Zhiping
Published in Bioorganic & medicinal chemistry letters (15.12.2010)
Published in Bioorganic & medicinal chemistry letters (15.12.2010)
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Journal Article
Discovery of novel pyridyl carboxamides as potent CCR5 antagonists and optimization of their pharmacokinetic profile in rats
Duan, Maosheng, Kazmierski, Wieslaw M., Chong, Pek Y., DeAnda, Felix, Edelstein, Mark, Ferris, Rob, Peckham, Jennifer, Wheelan, Pat, Xiong, Zhiping, Zhang, Huichang, Nishizawa, Rena, Takaoka, Yoshikazu
Published in Bioorganic & medicinal chemistry letters (01.11.2011)
Published in Bioorganic & medicinal chemistry letters (01.11.2011)
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