Zobrazeno 1 - 10
of 139
pro vyhledávání: '"F George, Njoroge"'
Autor:
Song Huang, Jason D. Graci, Paul Ingravallo, Anthony Turpoff, Neil Gregory Almstead, John Pichardo, Nanjing Zhang, Joseph M. Colacino, F. George Njoroge, Yalei Liu, Zhengxian Gu, Marla Weetall, Frederick C. Lahser, Stephen P. Jung, Gary Mitchell Karp, Amin A. Nomeir, Xiaoyan Zhang
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 26:594-601
A novel series of 2-(4-sulfonamidophenyl)-indole 3-carboxamides was identified and optimized for activity against the HCV genotype 1b replicon resulting in compounds with potent and selective activity. Further evaluation of this series demonstrated p
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::99f2dde02f0aa0ffaf8e4d127e01fcf0
https://doi.org/10.1016/j.bmcl.2015.11.065
https://doi.org/10.1016/j.bmcl.2015.11.065
Autor:
Pinto Patrick A, F. George Njoroge, Joseph A. Kozlowski, K.-C. Cheng, Hsueh-Cheng Huang, Frank Bennet, Tin-Yau Chan, Oleg Selyutin, Sony Agrawal, Yuhua Huang, Bancha Vibulbhan, Francisco Velazquez, Stuart B. Rosenblum, Srikanth Venkatraman, Yueheng Jiang, Gopinadhan N. Anilkumar, Cheng Li, Kevin X. Chen, Qingbei Zeng, Charles A. Lesburg, Neng-Yang Shih
Publikováno v:
ACS Medicinal Chemistry Letters. 5:244-248
Starting from indole-based hepatitis C virus (HCV) NS5B polymerase inhibitor lead compound 1, structure modifications were performed at multiple indole substituents to improve potency and pharmacokinetic (PK) properties. Bicyclic quinazolinone was fo
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::56d6b7cd7274b7db5b44ce371671e837
https://doi.org/10.1021/ml400192w
https://doi.org/10.1021/ml400192w
Autor:
Yalei Liu, Valerie Clausen, Amin A. Nomeir, Xiaoyan Zhang, Christie Morrill, William Joseph Lennox, Anthony Turpoff, Zhengxian Gu, Takashi Komatsu, Christine Espiritu, Neil Gregory Almstead, F. George Njoroge, Gary Mitchell Karp, Guangming Chen, Steven D. Paget, Joseph M. Colacino, Hongyu Ren, Chunshi Li, Jin Zhu, Jason D. Graci, Nanjing Zhang, Nicole Risher, Frederick C. Lahser, Marla Weetall, James J. Takasugi
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 23:3947-3953
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 culture assay. Preliminary optimization of this series furnished compounds with low nanomolar
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::b7637387fd6f4b0f3d5c90b600082ee8
https://doi.org/10.1016/j.bmcl.2013.04.049
https://doi.org/10.1016/j.bmcl.2013.04.049
Autor:
Stuart B. Rosenblum, Stephen Gavalas, Francisco Velazquez, Pinto Patrick A, Oleg Selyutin, Neng-Yang Shih, Yuhua Huang, Wanli Wu, Sony Agrawal, Yueheng Jiang, Srikanth Venkatraman, Joseph A. Kozlowski, Chuan-kui Jiang, Hsueh-Cheng Huang, Jose S. Duca, Anilkumar G. Nair, Bancha Vibulbhan, Eric Ferrari, Kevin X. Chen, Cheng Li, Charles A. Lesburg, F. George Njoroge, Frank Bennett, Qingbei Zeng
Publikováno v:
Bioorganic & Medicinal Chemistry. 21:2007-2017
The characterization of HCV genome has identified various vital functional proteins involved in the life cycle of hepatitis C virus. This has resulted in many novel enzymatic targets that are potential for development of therapeutic agents. The HCV R
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::f016854d014a0a4d91a3500623598032
https://doi.org/10.1016/j.bmc.2013.01.024
https://doi.org/10.1016/j.bmc.2013.01.024
Autor:
Ashok Arasappan, Seong-Heon Kim, Robert C. Reynolds, Cheng Li, Aneta Kosinski, Jeremy Clark, Joseph A. Kozlowski, Ling Tong, Vinay Girijavallabhan, Pinto Patrick A, Lei Chen, F. George Njoroge, Anita T. Fowler, Vishal Verma, Subramaniam Ananthan, Randall R. Rossman, Robert Chase, Neng-Yang Shih, Joseph A. Maddry, John A. Secrist, Cecil D. Kwong, Hollis S. Kezar, Abhijit Roychowdhury, Stephanie Curry, Malcolm MacCoss, Hsueh-Cheng Huang, Razia Rizvi, Frank Bennett, Stephen Gavalas, Yuhua Huang, Francisco Velazquez, Alvarez Carmen S, Feng Geng, Xiao Tong, John J. Piwinski, Regina Huelgas, Bandarpalle B. Shankar, Srikanth Venkatraman
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 22:3229-3234
Based on a previously identified HCV replication (replicase) inhibitor 1 , SAR efforts were conducted around the pyrimidine core to improve the potency and pharmacokinetic profile of the inhibitors. A benzothiazole moiety was found to be the optimal
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::63e593455015b9cae754dc9b1385747b
https://doi.org/10.1016/j.bmcl.2012.03.036
https://doi.org/10.1016/j.bmcl.2012.03.036
Autor:
Neng-Yang Shih, Joseph A. Maddry, Xiao Tong, Subramaniam Ananthan, Cheng Li, Jeremy Clark, Feng Geng, Hollis S. Kezar, Cecil D. Kwong, John J. Piwinski, Abhijit Roychowdhury, Robert C. Reynolds, Anita T. Fowler, Ashok Arasappan, Hsueh-Cheng Huang, John A. Secrist, F. George Njoroge, Boris Feld
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 22:1160-1164
Compound 1 was identified as a HCV replication inhibitor from screening/early SAR triage. Potency improvement was achieved via modulation of substituent on the 5-azo linkage. Due to potential toxicological concern, the 5-azo linkage was replaced with
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::5a01a2091efa205ec0a5d00edbf54a02
https://doi.org/10.1016/j.bmcl.2011.11.091
https://doi.org/10.1016/j.bmcl.2011.11.091
Autor:
Weing Yang, Bancha Vibulbhan, Neng-Yang Shih, Yuhua Huang, Latha G. Nair, Doll Ronald J, Kevin X. Chen, Stephane L. Bogen, F. George Njoroge, Frank Bennett
Publikováno v:
Tetrahedron Letters. 51:3057-3061
The Hepatitis C Virus (HCV) is a major health hazard and its infection is a leading cause of chronic liver disease world wide. In our efforts toward the discovery of a back up to our first clinical candidate, Boceprevir (SCH 503034), we approached th
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::5de2ab61d01e2f715b67efa13cdbe582
https://doi.org/10.1016/j.tetlet.2010.04.010
https://doi.org/10.1016/j.tetlet.2010.04.010
Autor:
Srikanth Venkatraman, Wanli Wu, Melissa Blackman, F. George Njoroge, Vincent Madison, Francisco Velazquez
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 20:2151-2155
Blood borne hepatitis C infections are the primary cause for liver cirrhosis and hepatocellular carcinoma. HCV NS3 protease, a pivotal enzyme in the replication cycle of HCV virus has been the primary target for development of new drug candidates. Bo
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::f9b3fa4a6e2dc78b50e86aca9729c684
https://doi.org/10.1016/j.bmcl.2010.02.051
https://doi.org/10.1016/j.bmcl.2010.02.051
Autor:
Hendrata Siska, Frank Bennett, Xiao Tong, Francisco Velazquez, Regina Huelgas, Kuo-Chi Cheng, Srikanth Venkatraman, Yuhua Huang, Andrew T. McPhail, Melissa Blackman, Patrick Pinto, Mousumi Sannigrahi, F. George Njoroge, Stephane L. Bogen, Raymond G. Lovey, Latha G. Nair, Ashok Arasappan
Publikováno v:
Journal of Medicinal Chemistry. 53:3075-3085
HCV infection affects more than 170 million people worldwide and many of those patients will reach the end stage complications of the disease which include hepatocarcinoma and liver failure. The success rate for treatment of patients infected with ge
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::7959a2ceb03f921c63714ac55e4f05e7
https://doi.org/10.1021/jm9016027
https://doi.org/10.1021/jm9016027
Publikováno v:
Tetrahedron Letters. 51:1276-1279
An efficient route for the synthesis of sterically hindered substituted and unsubstituted 2,6-dioxo tetrahydropyrimidines from amine 1 is described. These analogs are active against HCV NS3 serine protease. The biological data for some of the represe
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::007c8991d859a78b5a665f7ae1888d46
https://doi.org/10.1016/j.tetlet.2009.12.129
https://doi.org/10.1016/j.tetlet.2009.12.129