Search Results - "Njoroge, F. George"

Regioselective Cobalt-Catalyzed Addition of Sulfides to Unactivated Alkenes by Girijavallabhan, Vinay, Alvarez, Carmen, Njoroge, F. George

“…A novel method to synthesize tertiary alkyl/aryl sulfides in a mild and regioselective manner from unactivated alkenes using cobalt catalysis is described. The…”
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Challenges in Modern Drug Discovery: A Case Study of Boceprevir, an HCV Protease Inhibitor for the Treatment of Hepatitis C Virus Infection by Njoroge, F. George, Chen, Kevin X, Shih, Neng-Yang, Piwinski, John J

“…More than 170 million people worldwide are affected by the hepatitis C virus (HCV). The disease has been described as a “silent epidemic” and “a serious global…”
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Discovery of novel HCV inhibitors: Synthesis and biological activity of 6-(indol-2-yl)pyridine-3-sulfonamides targeting hepatitis C virus NS4B by Zhang, Xiaoyan, Zhang, Nanjing, Chen, Guangming, Turpoff, Anthony, Ren, Hongyu, Takasugi, James, Morrill, Christie, Zhu, Jin, Li, Chunshi, Lennox, William, Paget, Steven, Liu, Yalei, Almstead, Neil, George Njoroge, F., Gu, Zhengxian, Komatsu, Takashi, Clausen, Valerie, Espiritu, Christine, Graci, Jason, Colacino, Joseph, Lahser, Fred, Risher, Nicole, Weetall, Marla, Nomeir, Amin, Karp, Gary M.

“…A novel series of 6-(indol-2-yl)pyridine-3-sulfonamides was prepared and evaluated for their ability to inhibit HCV RNA replication in the HCV replicon cell…”
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Enantioselective Synthesis of 3,3-Difluoropyrrolidin-4-ol, a Valuable Building Block in Medicinal Chemistry by Si, Chong, Fales, Kevin R, Torrado, Alicia, Frimpong, Kwame, Kaoudi, Talbi, Vandeveer, Harold George, Njoroge, F. George

“…In this paper, we report for the first time two enantioselective routes to 4,4-difluoropyrrolidin-3-ol, a valuable building block in medicinal chemistry. In…”
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Structure–Activity Relationship (SAR) Optimization of 6‑(Indol-2-yl)pyridine-3-sulfonamides: Identification of Potent, Selective, and Orally Bioavailable Small Molecules Targeting Hepatitis C (HCV) NS4B by Zhang, Nanjing, Zhang, Xiaoyan, Zhu, Jin, Turpoff, Anthony, Chen, Guangming, Morrill, Christie, Huang, Song, Lennox, William, Kakarla, Ramesh, Liu, Ronggang, Li, Chunshi, Ren, Hongyu, Almstead, Neil, Venkatraman, Srikanth, Njoroge, F. George, Gu, Zhengxian, Clausen, Valerie, Graci, Jason, Jung, Stephen P., Zheng, Yingcong, Colacino, Joseph M., Lahser, Fred, Sheedy, Josephine, Mollin, Anna, Weetall, Marla, Nomeir, Amin, Karp, Gary M.

“…A novel, potent, and orally bioavailable inhibitor of hepatitis C RNA replication targeting NS4B, compound 4t (PTC725), has been identified through chemical…”
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Potent inhibitors of HCV-NS3 protease derived from boronic acids by Venkatraman, Srikanth, Wu, Wanli, Prongay, Andrew, Girijavallabhan, Viyyoor, George Njoroge, F.

“…Chronic hepatitis C infection is the leading causes for cirrhosis of the liver and hepatocellular carcinoma, leading to liver failure and liver…”
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A notable conversion of a thiolacetate to its corresponding sulfonyl chloride by Huang, Yuhua, Bennett, Frank, Verma, Vishal, George Njoroge, F., MacCoss, Malcolm

“…A direct conversion of a thiolacetate to its corresponding sulfonyl chloride in the presence of acid and base sensitive functional groups is described…”
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Optimization of potency and pharmacokinetics of tricyclic indole derived inhibitors of HCV NS5B polymerase. Identification of ester prodrugs with improved oral pharmacokinetics by Venkatraman, Srikanth, Velazquez, Francisco, Gavalas, Stephen, Wu, Wanli, Chen, Kevin X., Nair, Anilkumar G., Bennett, Frank, Huang, Yuhua, Pinto, Patrick, Jiang, Yueheng, Selyutin, Oleg, Vibulbhan, Bancha, Zeng, Qingbei, Lesburg, Charles, Duca, Jose, Heimark, Larry, Huang, Hsueh-Cheng, Agrawal, Sony, Jiang, Chuan-kui, Ferrari, Eric, Li, Cheng, Kozlowski, Joseph, Rosenblum, Stuart, Shih, Neng-Yang, Njoroge, F. George

“…HCV infections are the leading causes for hepatocellular carcinoma and liver transplantation in the United States. Recent advances in drug discovery have…”
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Discovery of potent sulfonamide P4-capped ketoamide second generation inhibitors of hepatitis C virus NS3 serine protease with favorable pharmacokinetic profiles in preclinical species by Bogen, Stéphane L., Arasappan, Ashok, Velazquez, Francisco, Blackman, Melissa, Huelgas, Regina, Pan, Weidong, Siegel, Elise, Nair, Latha G., Venkatraman, Srikanth, Guo, Zhuyan, Doll, Ronald, Shih, Neng-Yang, George Njoroge, F.

“…Hepatitis is a disease characterized by inflammation of the liver, usually producing swelling and, in many cases, permanent damage to liver tissues. Viral…”
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II. Novel HCV NS5B polymerase inhibitors: Discovery of indole C2 acyl sulfonamides by Anilkumar, Gopinadhan N., Selyutin, Oleg, Rosenblum, Stuart B., Zeng, Qingbei, Jiang, Yueheng, Chan, Tin-Yau, Pu, Haiyan, Wang, Li, Bennett, Frank, Chen, Kevin X., Lesburg, Charles A., Duca, Jose, Gavalas, Stephen, Huang, Yuhua, Pinto, Patrick, Sannigrahi, Mousumi, Velazquez, Francisco, Venkatraman, Srikanth, Vibulbhan, Bancha, Agrawal, Sony, Ferrari, Eric, Jiang, Chuan-kui, Huang, H.-C., Shih, Neng-Yang, George Njoroge, F., Kozlowski, Joseph A.

“…Development of SAR at the C2 position of indole lead 1, a palm site inhibitor of HCV NS5B polymerase (NS5B IC50=0.053μM, replicon EC50=4.8μM), is described…”
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5-Benzothiazole substituted pyrimidine derivatives as HCV replication (replicase) inhibitors by Arasappan, Ashok, Bennett, Frank, Girijavallabhan, Vinay, Huang, Yuhua, Huelgas, Regina, Alvarez, Carmen, Chen, Lei, Gavalas, Stephen, Kim, Seong-Heon, Kosinski, Aneta, Pinto, Patrick, Rizvi, Razia, Rossman, Randall, Shankar, Bandarpalle, Tong, Ling, Velazquez, Francisco, Venkatraman, Srikanth, Verma, Vishal A., Kozlowski, Joseph, Shih, Neng-Yang, Piwinski, John J., MacCoss, Malcolm, Kwong, Cecil D., Clark, Jeremy L., Fowler, Anita T., Geng, Feng, Kezar, Hollis S., Roychowdhury, Abhijit, Reynolds, Robert C., Maddry, Joseph A., Ananthan, Subramaniam, Secrist, John A., Li, Cheng, Chase, Robert, Curry, Stephanie, Huang, Hsueh-Cheng, Tong, Xiao, Njoroge, F. George

“…Based on a previously identified HCV replication (replicase) inhibitor 1, SAR efforts were conducted around the pyrimidine core to improve the potency and…”
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Novel substituted pyrimidines as HCV replication (replicase) inhibitors by Kwong, Cecil D., Clark, Jeremy L., Fowler, Anita T., Geng, Feng, Kezar, Hollis S., Roychowdhury, Abhijit, Reynolds, Robert C., Maddry, Joseph A., Ananthan, Subramaniam, Secrist, John A., Shih, Neng-Yang, Piwinski, John J., Li, Cheng, Feld, Boris, Huang, Hsueh-Cheng, Tong, Xiao, George Njoroge, F., Arasappan, Ashok

“…Compound 1 was identified as a HCV replication inhibitor from screening/early SAR triage. Potency improvement was achieved via modulation of substituent on the…”
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Synthesis and SAR of pyridothiazole substituted pyrimidine derived HCV replication inhibitors by Girijavallabhan, Vinay M., Alvarez, Carmen, Bennett, Frank, Chen, Lei, Gavalas, Stephen, Huang, Yuhua, Kim, Seong-Heon, Kosinski, Aneta, Pinto, Patrick, Rizvi, Razia, Rossman, Randall, Shankar, Bandarpalle, Tong, Ling, Velazquez, Francisco, Venkatraman, Srikanth, Verma, Vishal A., Kozlowski, Joseph, Shih, Neng-Yang, Piwinski, John J., MacCoss, Malcolm, Kwong, Cecil D., Bansal, Namita, Clark, Jeremy L., Fowler, Anita T., Kezar, Hollis S., Valiyaveettil, Jacob, Reynolds, Robert C., Maddry, Joseph A., Ananthan, Subramaniam, Secrist, John A., Li, Cheng, Chase, Robert, Curry, Stephanie, Huang, Hsueh-Cheng, Tong, Xiao, Njoroge, F. George, Arasappan, Ashok

“…Introduction of a nitrogen atom into the benzene ring of a previously identified HCV replication (replicase) benzothiazole inhibitor 1, resulted in the…”
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Potent aza-peptide derived inhibitors of HCV NS3 protease by Venkatraman, Srikanth, Wu, Wanli, Shih, Neng-Yang, George Njoroge, F.

“…Chronic hepatitis C infection is the primary cause for cirrhosis of the liver and hepatocellular carcinoma leading to liver failure and transplantation. The…”
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P4 capped amides and lactams as HCV NS3 protease inhibitors with improved potency and DMPK profile by Nair, Latha G., Sannigrahi, Mousumi, Bogen, Stephane, Pinto, Patrick, Chen, Kevin X., Prongay, Andrew, Tong, Xiao, Cheng, K.-C., Girijavallabhan, Viyyoor, George Njoroge, F.

“…SAR studies on the extension of P3 unit of Boceprevir ( 1, SCH 503034) with amides and lactams and their synthesis is described. SAR studies on the extension…”
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Pyridofuran substituted pyrimidine derivatives as HCV replication (replicase) inhibitors by Bennett, Frank, Kezar, Hollis S., Girijavallabhan, Vinay, Huang, Yuhua, Huelgas, Regina, Rossman, Randall, Shih, Neng-Yang, Piwinski, John J., MacCoss, Malcolm, Kwong, Cecil D., Clark, Jeremy L., Fowler, Anita T., Geng, Feng, Roychowdhury, Abhijit, Reynolds, Robert C., Maddry, Joseph A., Ananthan, Subramaniam, Secrist, John A., Li, Cheng, Chase, Robert, Curry, Stephanie, Huang, Hsueh-Cheng, Tong, Xiao, George Njoroge, F., Arasappan, Ashok

“…Introduction of nitrogen atom into the benzene ring of a previously identified HCV replication (replicase) benzofuran inhibitor 2, resulted in the discovery of…”
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Impact of Naturally Occurring Variants of HCV Protease on the Binding of Different Classes of Protease Inhibitors by Tong, Xiao, Guo, Zhuyan, Wright-Minogue, Jacquelyn, Xia, Ellen, Prongay, Andrew, Madison, Vincent, Qiu, Ping, Venkatraman, Srikanth, Velazquez, Francisco, Njoroge, F. George, Malcolm, Bruce A.

“…HCV drug discovery efforts have largely focused on genotype 1 virus due to its prevalence and relatively poor response to current therapy. However, patients…”
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Ultra-performance liquid chromatography/tandem mass spectrometric determination of diastereomers of SCH 503034 in monkey plasma by Wang, Ganfeng, Hsieh, Yunsheng, Cheng, Kuo-Chi, Morrison, Richard A., Venkatraman, Srikanth, Njoroge, F. George, Heimark, Larry, Korfmacher, Walter A.

“…This paper describes the development and qualification of a fast, sensitive and specific ultra-performance liquid chromatography/tandem mass spectrometric…”
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Discovery of N‑(6-Fluoro-1-oxo-1,2-dihydroisoquinolin-7-yl)-5-[(3R)‑3-hydroxypyrrolidin-1-yl]­thiophene-2-sulfonamide (LSN 3213128), a Potent and Selective Nonclassical Antifolate Aminoimidazole-4-carboxamide Ribonucleotide Formyltransferase (AICARFT) Inhibitor Effective at Tumor Suppression in a Cancer Xenograft Model by Fales, Kevin R., Njoroge, F. George, Brooks, Harold B., Thibodeaux, Stefan, Torrado, Alicia, Si, Chong, Toth, James L., Mc Cowan, Jefferson R., Roth, Kenneth D., Thrasher, Kenneth J., Frimpong, Kwame, Lee, Matthew R., Dally, Robert D., Shepherd, Timothy A., Durham, Timothy B., Margolis, Brandon J., Wu, Zhipei, Wang, Yong, Atwell, Shane, Wang, Jing, Hui, Yu-Hua, Meier, Timothy I., Konicek, Susan A., Geeganage, Sandaruwan

“…A hallmark of cancer is unbridled proliferation that can result in increased demand for de novo synthesis of purine and pyrimidine bases required for DNA and…”
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An efficient synthesis of 3,4-dihydropyridone via a tandem olefin isomerization–ring-closing metathesis reaction by Si, Chong, Fales, Kevin R., Boyer, Robert D., George Njoroge, F.

“…•An efficient methodology to prepare 3,4-dihydropyridones was developed.•A tandem olefin isomerization–ring-closing metathesis mechanism was…”
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