Search Results - "Swidorski, Jacob J."

A Concise Total Synthesis of (−)-Cylindricine C through a Stereoselective Intramolecular Aza-[3 + 3] Annulation Strategy by Swidorski, Jacob J, Wang, Jiashi, Hsung, Richard P

“…An enantioselective total synthesis of (−)-cylindricine C is described, featuring a diastereoselective intramolecular aza-[3 + 3] annulation strategy and an…”
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An N-Acyliminium Cyclization Approach to a Total Synthesis of (+)-Cylindricine C by Liu, Jia, Swidorski, Jacob J, Peters, Scott D, Hsung, Richard P

“…Details of problems and solutions encountered during the development of an enantioselective total synthesis of (+)-cylindricine C are described here. The total…”
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Atropisomerism Observed in Galactose-Based Monosaccharide Inhibitors of Galectin-3 Comprising 2-Methyl-4-phenyl-2,4-dihydro-3 H -1,2,4-triazole-3-thione by Yoon, David S, Liu, Chunjian, Jalagam, Prasada Rao, Feng, Jianxin, Wang, Wei, Swidorski, Jacob J, Xu, Li, Hartz, Richard A, Nair, Satheesh K, Beno, Brett R, Panda, Manoranjan, Ghosh, Kaushik, Kumar, Amit, Sale, Harinath, Shah, Devang, Mathur, Arvind, Ellsworth, Bruce A, Cheng, Dong, Regueiro-Ren, Alicia

“…Galectin-3 (Gal-3) is a carbohydrate binding protein that has been implicated in the development and progression of fibrotic diseases. Proof-of-principal…”
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Atropisomerism Observed in Galactose-Based Monosaccharide Inhibitors of Galectin‑3 Comprising 2‑Methyl-4-phenyl-2,4-dihydro‑3H‑1,2,4-triazole-3-thione by Yoon, David S., Liu, Chunjian, Jalagam, Prasada Rao, Feng, Jianxin, Wang, Wei, Swidorski, Jacob J., Xu, Li, Hartz, Richard A., Nair, Satheesh K., Beno, Brett R., Panda, Manoranjan, Ghosh, Kaushik, Kumar, Amit, Sale, Harinath, Shah, Devang, Mathur, Arvind, Ellsworth, Bruce A., Cheng, Dong, Regueiro-Ren, Alicia

“…Galectin-3 (Gal-3) is a carbohydrate binding protein that has been implicated in the development and progression of fibrotic diseases. Proof-of-principal…”
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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 by 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

“…BMS-955176 is a second-generation human immunodeficiency virus type 1 (HIV-1) maturation inhibitor (MI). A first-generation MI, bevirimat, showed clinical…”
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The Discovery of GSK3640254, a Next-Generation Inhibitor of HIV‑1 Maturation by 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

“…GSK3640254 is an HIV-1 maturation inhibitor (MI) that exhibits significantly improved antiviral activity toward a range of clinically relevant polymorphic…”
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Design and exploration of C-3 benzoic acid bioisosteres and alkyl replacements in the context of GSK3532795 (BMS-955176) that exhibit broad spectrum HIV-1 maturation inhibition by Swidorski, Jacob J., Jenkins, Susan, Hanumegowda, Umesh, Parker, Dawn D., Beno, Brett R., Protack, Tricia, Ng, Alicia, Gupta, Anuradha, Shanmugam, Yoganand, Dicker, Ira B., Krystal, Mark, Meanwell, Nicholas A., Regueiro-Ren, Alicia

“…[Display omitted] GSK3532795 (formerly BMS-955176) is a second-generation HIV-1 maturation inhibitor that has shown broad spectrum antiviral activity and…”
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The design, synthesis and structure-activity relationships associated with C28 amine-based betulinic acid derivatives as inhibitors of HIV-1 maturation by 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

“…[Display omitted] The design and synthesis of a series of C28 amine-based betulinic acid derivatives as HIV-1 maturation inhibitors is described. This series…”
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Discovery and exploration of monosaccharide linked dimers of galectin-3 inhibitors to target fibrosis by Swidorski, Jacob J., Beno, Brett R., Liu, Chunjian, Yoon, David S., Ghosh, Kaushik, Sale, Harinath, Shah, Devang, Acharya, Kriti, Yanchunas, Joseph, Haldar, Priyanka, Kalidindi, Narasimharaju, Shukla, Jinal K., Argentieri, Matthew, Ellsworth, Bruce A., Cheng, Dong, Regueiro-Ren, Alicia

“…Galectin proteins have been targets of interest in numerous therapeutic areas for some time. Galectin-3 has been identified as a target of particular interest…”
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Inhibitors of HIV-1 attachment: The discovery and structure–activity relationships of tetrahydroisoquinolines as replacements for the piperazine benzamide in the 3-glyoxylyl 6-azaindole pharmacophore by Swidorski, Jacob J., Liu, Zheng, Yin, Zhiwei, Wang, Tao, Carini, David J., Rahematpura, Sandhya, Zheng, Ming, Johnson, Kim, Zhang, Sharon, Lin, Pin-Fang, Parker, Dawn D., Li, Wenying, Meanwell, Nicholas A., Hamann, Lawrence G., Regueiro-Ren, Alicia

“…[Display omitted] 6,6-Fused ring systems including tetrahydroisoquinolines and tetrahydropyrido[3,4-d]pyrimidines have been explored as possible replacements…”
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Inhibitors of Human Immunodeficiency Virus Type 1 (HIV-1) Attachment. 12. Structure–Activity Relationships Associated with 4‑Fluoro-6-azaindole Derivatives Leading to the Identification of 1‑(4-Benzoylpiperazin-1-yl)-2-(4-fluoro-7-[1,2,3]triazol-1-yl‑1H‑pyrrolo[2,3‑c]pyridin-3-yl)ethane-1,2-dione (BMS-585248) by Regueiro-Ren, Alicia, Xue, Qiufen M, Swidorski, Jacob J, Gong, Yi-Fei, Mathew, Marina, Parker, Dawn D, Yang, Zheng, Eggers, Betsy, D’Arienzo, Celia, Sun, Yongnian, Malinowski, Jacek, Gao, Qi, Wu, Dedong, Langley, David R, Colonno, Richard J, Chien, Caly, Grasela, Dennis M, Zheng, Ming, Lin, Pin-Fang, Meanwell, Nicholas A, Kadow, John F

“…A series of highly potent HIV-1 attachment inhibitors with 4-fluoro-6-azaindole core heterocycles that target the viral envelope protein gp120 has been…”
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Inhibitors of HIV-1 maturation: Development of structure–activity relationship for C-28 amides based on C-3 benzoic acid-modified triterpenoids by 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

“…[Display omitted] We have recently reported on the discovery of a C-3 benzoic acid (1) as a suitable replacement for the dimethyl succinate side chain of…”
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C-3 benzoic acid derivatives of C-3 deoxybetulinic acid and deoxybetulin as HIV-1 maturation inhibitors by Liu, Zheng, Swidorski, Jacob J., Nowicka-Sans, Beata, Terry, Brian, Protack, Tricia, Lin, Zeyu, Samanta, Himadri, Zhang, Sharon, Li, Zhufang, Parker, Dawn D., Rahematpura, Sandhya, Jenkins, Susan, Beno, Brett R., Krystal, Mark, Meanwell, Nicholas A., Dicker, Ira B., Regueiro-Ren, Alicia

“…[Display omitted] A series of C-3 phenyl- and heterocycle-substituted derivatives of C-3 deoxybetulinic acid and C-3 deoxybetulin was designed and synthesized…”
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Microbial transformations of betulinic and betulonic acids by Goswami, Animesh, Guo, Zhiwei, Tully, Thomas P., Rinaldi, Frank A., Huang, Xiaohua Stella, Swidorski, Jacob J., Regueiro-Ren, Alicia

“…•Enzymatic oxidations of betulinic and betulonic acids.•Biotransformations with two bacteria and two fungi were studied.•Several di-, tri-, tetrahydroxy and…”
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Discovery of BMS-955176, a Second Generation HIV‑1 Maturation Inhibitor with Broad Spectrum Antiviral Activity by 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

“…HIV-1 maturation inhibition (MI) has been clinically validated as an approach to the control of HIV-1 infection. However, identifying an MI with both broad…”
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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) by 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

“…GSK3532795, formerly known as BMS-955176 (1), is a potent, orally active, second-generation HIV-1 maturation inhibitor (MI) that advanced through phase IIb…”
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A Lewis Acid-Catalyzed Formal [3 + 3] Cycloaddition of α,β-Unsaturated Aldehydes with 4-Hydroxy-2-Pyrone, Diketones, and Vinylogous Esters by Kurdyumov, Aleksey V, Lin, Nan, Hsung, Richard P, Gullickson, Glen C, Cole, Kevin P, Sydorenko, Nadiya, Swidorski, Jacob J

“…A Lewis acid-catalyzed formal cycloaddition of α,β-unsaturated aldehydes with 6-methyl-4-hydroxy-2-pyrone, 1,3-diketones, and vinylogous silyl esters is…”
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An Efficient Assembly of Heterobenzazepine Ring Systems Utilizing an Intramolecular Palladium-Catalyzed Cycloamination by Margolis, Brandon J, Swidorski, Jacob J, Rogers, Bruce N

“…Azaheterocyclic compounds are interesting and medicinally relevant targets. Herein we disclose an improved synthesis into the oxazepine and thiazepine ring…”
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Design, Synthesis, and SAR of C‑3 Benzoic Acid, C‑17 Triterpenoid Derivatives. Identification of the HIV‑1 Maturation Inhibitor 4‑((1R,3aS,5aR,5bR,7aR,11aS,11bR,13aR,13bR)‑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‑1H‑cyclopenta[a]chrysen-9-yl)benzoic Acid (GSK3532795, BMS-955176) by 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.

“…GSK3532795, formerly known as BMS-955176 (1), is a potent, orally active, second-generation HIV-1 maturation inhibitor (MI) that advanced through phase IIb…”
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Invention of VH-937, a Potent HIV‑1 Maturation Inhibitor with the Potential for Infrequent Oral Dosing in Humans by Sit, Sing-Yuen, Chen, Yan, Chen, Jie, Venables, Brian L., Swidorski, Jacob J., Xu, Li, Sin, Ny, Hartz, Richard A., Lin, Zeyu, Zhang, Sharon, Li, Zhufang, Wu, Dauh-Rurng, Li, Peng, Kempson, James, Hou, Xiaoping, Shanmugam, Yoganand, Parker, Dawn, Jenkins, Susan, Simmermacher, Jean, Falk, Paul, McAuliffe, Brian, Cockett, Mark, Hanumegowda, Umesh, Dicker, Ira, Krystal, Mark, Meanwell, Nicholas A., Regueiro-Ren, Alicia

“…Newer generation HIV-1 maturation inhibitors have proven to be viable antiretroviral agents in the clinic. VH3739937, (VH-937, 24) is an advanced HIV-1…”
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