GSK3640254 Is a Novel HIV-1 Maturation Inhibitor with an Optimized Virology Profile
Dicker, Ira, Jeffrey, Jerry L, Protack, Tricia, Lin, Zeyu, Cockett, Mark, Chen, Yan, Sit, Sing-Yuen, Gartland, Martin, Meanwell, Nicholas A, Regueiro-Ren, Alicia, Drexler, Dieter, Cantone, Joseph, McAuliffe, Brian, Krystal, Mark
Published in Antimicrobial agents and chemotherapy (18.01.2022)
Published in Antimicrobial agents and chemotherapy (18.01.2022)
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Identification and Characterization of BMS-955176, a Second-Generation HIV-1 Maturation Inhibitor with Improved Potency, Antiviral Spectrum, and Gag Polymorphic Coverage
Nowicka-Sans, Beata, Protack, Tricia, Lin, Zeyu, Li, Zhufang, Zhang, Sharon, Sun, Yongnian, Samanta, Himadri, Terry, Brian, Liu, Zheng, Chen, Yan, Sin, Ny, Sit, Sing-Yuen, Swidorski, Jacob J, Chen, Jie, Venables, Brian L, Healy, Matthew, Meanwell, Nicholas A, Cockett, Mark, Hanumegowda, Umesh, Regueiro-Ren, Alicia, Krystal, Mark, Dicker, Ira B
Published in Antimicrobial agents and chemotherapy (01.07.2016)
Published in Antimicrobial agents and chemotherapy (01.07.2016)
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Synthesis, Structure–Activity Relationships, and In Vivo Evaluation of Novel C‑17 Amine Derivatives Based on GSK3640254 as HIV‑1 Maturation Inhibitors with Broad Spectrum Activity
Hartz, Richard A., Xu, Li, Sit, Sing-Yuen, Chen, Jie, Venables, Brian L., Lin, Zeyu, Zhang, Sharon, Li, Zhufang, Parker, Dawn, Simmons, Tara S., Jenkins, Susan, Hanumegowda, Umesh M., Dicker, Ira, Krystal, Mark, Meanwell, Nicholas A., Regueiro-Ren, Alicia
Published in Journal of medicinal chemistry (08.12.2022)
Published in Journal of medicinal chemistry (08.12.2022)
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Journal Article
The Discovery of GSK3640254, a Next-Generation Inhibitor of HIV‑1 Maturation
Regueiro-Ren, Alicia, Sit, Sing-Yuen, Chen, Yan, Chen, Jie, Swidorski, Jacob J., Liu, Zheng, Venables, Brian L., Sin, Ny, Hartz, Richard A., Protack, Tricia, Lin, Zeyu, Zhang, Sharon, Li, Zhufang, Wu, Dauh-Rurng, Li, Peng, Kempson, James, Hou, Xiaoping, Gupta, Anuradha, Rampulla, Richard, Mathur, Arvind, Park, Hyunsoo, Sarjeant, Amy, Benitex, Yulia, Rahematpura, Sandhya, Parker, Dawn, Phillips, Thomas, Haskell, Roy, Jenkins, Susan, Santone, Kenneth S., Cockett, Mark, Hanumegowda, Umesh, Dicker, Ira, Meanwell, Nicholas A., Krystal, Mark
Published in Journal of medicinal chemistry (22.09.2022)
Published in Journal of medicinal chemistry (22.09.2022)
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Discovery and Early Clinical Evaluation of BMS-605339, a Potent and Orally Efficacious Tripeptidic Acylsulfonamide NS3 Protease Inhibitor for the Treatment of Hepatitis C Virus Infection
Scola, Paul M., Wang, Alan Xiangdong, Good, Andrew C., Sun, Li-Qiang, Combrink, Keith D., Campbell, Jeffrey A., Chen, Jie, Tu, Yong, Sin, Ny, Venables, Brian L., Sit, Sing-Yuen, Chen, Yan, Cocuzza, Anthony, Bilder, Donna M., D’Andrea, Stanley, Zheng, Barbara, Hewawasam, Piyasena, Ding, Min, Thuring, Jan, Li, Jianqing, Hernandez, Dennis, Yu, Fei, Falk, Paul, Zhai, Guangzhi, Sheaffer, Amy K., Chen, Chaoqun, Lee, Min S., Barry, Diana, Knipe, Jay O., Li, Wenying, Han, Yong-Hae, Jenkins, Susan, Gesenberg, Christoph, Gao, Qi, Sinz, Michael W., Santone, Kenneth S., Zvyaga, Tatyana, Rajamani, Ramkumar, Klei, Herbert E., Colonno, Richard J., Grasela, Dennis M., Hughes, Eric, Chien, Caly, Adams, Stephen, Levesque, Paul C., Li, Danshi, Zhu, Jialong, Meanwell, Nicholas A., McPhee, Fiona
Published in Journal of medicinal chemistry (13.03.2014)
Published in Journal of medicinal chemistry (13.03.2014)
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The Discovery of Asunaprevir (BMS-650032), An Orally Efficacious NS3 Protease Inhibitor for the Treatment of Hepatitis C Virus Infection
Scola, Paul M., Sun, Li-Qiang, Wang, Alan Xiangdong, Chen, Jie, Sin, Ny, Venables, Brian L., Sit, Sing-Yuen, Chen, Yan, Cocuzza, Anthony, Bilder, Donna M., D’Andrea, Stanley V., Zheng, Barbara, Hewawasam, Piyasena, Tu, Yong, Friborg, Jacques, Falk, Paul, Hernandez, Dennis, Levine, Steven, Chen, Chaoqun, Yu, Fei, Sheaffer, Amy K., Zhai, Guangzhi, Barry, Diana, Knipe, Jay O., Han, Yong-Hae, Schartman, Richard, Donoso, Maria, Mosure, Kathy, Sinz, Michael W., Zvyaga, Tatyana, Good, Andrew C., Rajamani, Ramkumar, Kish, Kevin, Tredup, Jeffrey, Klei, Herbert E., Gao, Qi, Mueller, Luciano, Colonno, Richard J., Grasela, Dennis M., Adams, Stephen P., Loy, James, Levesque, Paul C., Sun, Huabin, Shi, Hong, Sun, Lucy, Warner, William, Li, Danshi, Zhu, Jialong, Meanwell, Nicholas A., McPhee, Fiona
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 Profile of the HIV-1 Maturation Inhibitor VH3739937
McAuliffe, Brian, Falk, Paul, Chen, Jie, Chen, Yan, Sit, Sing-Yuen, Swidorski, Jacob, Hartz, Richard A, Xu, Li, Venables, Brian, Sin, Ny, Meanwell, Nicholas A, Regueiro-Ren, Alicia, Wensel, David, Hanumegowda, Umesh, Krystal, Mark
Published in Viruses (24.09.2024)
Published in Viruses (24.09.2024)
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Journal Article
The design, synthesis and structure-activity relationships associated with C28 amine-based betulinic acid derivatives as inhibitors of HIV-1 maturation
Chen, Yan, Sit, Sing-Yuen, Chen, Jie, Swidorski, Jacob J., Liu, Zheng, Sin, Ny, Venables, Brian L., Parker, Dawn D., Nowicka-Sans, Beata, Lin, Zeyu, Li, Zhufang, Terry, Brian J., Protack, Tricia, Rahematpura, Sandhya, Hanumegowda, Umesh, Jenkins, Susan, Krystal, Mark, Dicker, Ira D., Meanwell, Nicholas A., Regueiro-Ren, Alicia
Published in Bioorganic & medicinal chemistry letters (15.05.2018)
Published in Bioorganic & medicinal chemistry letters (15.05.2018)
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Journal Article
Discovery of new indole-based acylsulfonamide Nav1.7 inhibitors
Wu, Yong-Jin, Venables, Brian, Guernon, Jason, Chen, Jie, Sit, Sing-Yuen, Rajamani, Ramkumar, Knox, Ronald J., Matchett, Michele, Pieschl, Rick L., Herrington, James, Bristow, Linda J., Meanwell, Nicholas A., Thompson, Lorin A., Dzierba, Carolyn
Published in Bioorganic & medicinal chemistry letters (15.02.2019)
Published in Bioorganic & medicinal chemistry letters (15.02.2019)
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Journal Article
Inhibitors of HIV-1 maturation: Development of structure–activity relationship for C-28 amides based on C-3 benzoic acid-modified triterpenoids
Swidorski, Jacob J., Liu, Zheng, Sit, Sing-Yuen, Chen, Jie, Chen, Yan, Sin, Ny, Venables, Brian L., Parker, Dawn D., Nowicka-Sans, Beata, Terry, Brian J., Protack, Tricia, Rahematpura, Sandhya, Hanumegowda, Umesh, Jenkins, Susan, Krystal, Mark, Dicker, Ira B., Meanwell, Nicholas A., Regueiro-Ren, Alicia
Published in Bioorganic & medicinal chemistry letters (15.04.2016)
Published in Bioorganic & medicinal chemistry letters (15.04.2016)
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Journal Article
Discovery of BMS-955176, a Second Generation HIV‑1 Maturation Inhibitor with Broad Spectrum Antiviral Activity
Regueiro-Ren, Alicia, Liu, Zheng, Chen, Yan, Sin, Ny, Sit, Sing-Yuen, Swidorski, Jacob J, Chen, Jie, Venables, Brian L, Zhu, Juliang, Nowicka-Sans, Beata, Protack, Tricia, Lin, Zeyu, Terry, Brian, Samanta, Himadri, Zhang, Sharon, Li, Zhufang, Beno, Brett R, Huang, Xiaohua S, Rahematpura, Sandhya, Parker, Dawn D, Haskell, Roy, Jenkins, Susan, Santone, Kenneth S, Cockett, Mark I, Krystal, Mark, Meanwell, Nicholas A, Hanumegowda, Umesh, Dicker, Ira B
Published in ACS medicinal chemistry letters (09.06.2016)
Published in ACS medicinal chemistry letters (09.06.2016)
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Journal Article
Design, Synthesis, and SAR of C-3 Benzoic Acid, C-17 Triterpenoid Derivatives. Identification of the HIV-1 Maturation Inhibitor 4-((1 R,3a S,5a R,5b R,7a R,11a S,11b R,13a R,13b R)-3a-((2-(1,1-Dioxidothiomorpholino)ethyl)amino)-5a,5b,8,8,11a-pentamethyl-1-(prop-1-en-2-yl)-2,3,3a,4,5,5a,5b,6,7,7a,8,11,11a,11b,12,13,13a,13b-octadecahydro-1 H-cyclopenta[ a]chrysen-9-yl)benzoic Acid (GSK3532795, BMS-955176)
Regueiro-Ren, Alicia, Swidorski, Jacob J, Liu, Zheng, Chen, Yan, Sin, Ny, Sit, Sing-Yuen, Chen, Jie, Venables, Brian L, Zhu, Juliang, Nowicka-Sans, Beata, Protack, Tricia, Lin, Zeyu, Terry, Brian, Samanta, Himadri, Zhang, Sharon, Li, Zhufang, Easter, John, Beno, Brett R, Arora, Vinod, Huang, Xiaohua S, Rahematpura, Sandhya, Parker, Dawn D, Haskell, Roy, Santone, Kenneth S, Cockett, Mark I, Krystal, Mark, Meanwell, Nicholas A, Jenkins, Susan, Hanumegowda, Umesh, Dicker, Ira B
Published in Journal of medicinal chemistry (23.08.2018)
Published in Journal of medicinal chemistry (23.08.2018)
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Journal Article
Discovery of a Potent Acyclic, Tripeptidic, Acyl Sulfonamide Inhibitor of Hepatitis C Virus NS3 Protease as a Back-up to Asunaprevir with the Potential for Once-Daily Dosing
Sun, Li-Qiang, Mull, Eric, Zheng, Barbara, D’Andrea, Stanley, Zhao, Qian, Wang, Alan Xiangdong, Sin, Ny, Venables, Brian L, Sit, Sing-Yuen, Chen, Yan, Chen, Jie, Cocuzza, Anthony, Bilder, Donna M, Mathur, Arvind, Rampulla, Richard, Chen, Bang-Chi, Palani, Theerthagiri, Ganesan, Sivakumar, Arunachalam, Pirama Nayagam, Falk, Paul, Levine, Steven, Chen, Chaoqun, Friborg, Jacques, Yu, Fei, Hernandez, Dennis, Sheaffer, Amy K, Knipe, Jay O, Han, Yong-Hae, Schartman, Richard, Donoso, Maria, Mosure, Kathy, Sinz, Michael W, Zvyaga, Tatyana, Rajamani, Ramkumar, Kish, Kevin, Tredup, Jeffrey, Klei, Herbert E, Gao, Qi, Ng, Alicia, Mueller, Luciano, Grasela, Dennis M, Adams, Stephen, Loy, James, Levesque, Paul C, Sun, Huabin, Shi, Hong, Sun, Lucy, Warner, William, Li, Danshi, Zhu, Jialong, Wang, Ying-Kai, Fang, Hua, Cockett, Mark I, Meanwell, Nicholas A, McPhee, Fiona, Scola, Paul M
Published in Journal of medicinal chemistry (08.09.2016)
Published in Journal of medicinal chemistry (08.09.2016)
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3-Thio-quinolinone maxi-K openers for the treatment of erectile dysfunction
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Sit, Sing-Yuen, Xie, Kai, Jacutin-Porte, Swanee, Boy, Kenneth M, Seanz, James, Taber, Matthew T, Gulwadi, Amit G, Korpinen, Carolyn D, Burris, Kevin D, Molski, Thaddeus F, Ryan, Elaine, Xu, Cen, Verdoorn, Todd, Johnson, Graham, Nichols, David E, Mailman, Richard B
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