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Structure-activity relationships of proline modifications around the tetracyclic-indole class of NS5A inhibitors.
Tong, Ling; Yu, Wensheng; Coburn, Craig A; Chen, Lei; Selyutin, Oleg; Zeng, Qingbei; Dwyer, Michael P; Nair, Anilkumar G; Shankar, Bandarpalle B; Kim, Seong Heon; Yang, De-Yi; Rosenblum, Stuart B; Ruck, Rebecca T; Davies, Ian W; Hu, Bin; Zhong, Bin; Hao, Jinglai; Ji, Tao; Zan, Shuai; Liu, Rong; Agrawal, Sony; Carr, Donna; Curry, Stephanie; McMonagle, Patricia; Bystol, Karin; Lahser, Frederick; Ingravallo, Paul; Chen, Shiying; Asante-Appiah, Ernest; Kozlowski, Joseph A.
Afiliação
  • Tong L; Merck & Co., Inc., 126 E. Lincoln Ave., Rahway, NJ 07065, USA. Electronic address: ling.tong@merck.com.
  • Yu W; Merck & Co., Inc., 126 E. Lincoln Ave., Rahway, NJ 07065, USA.
  • Coburn CA; Merck & Co., Inc., 126 E. Lincoln Ave., Rahway, NJ 07065, USA.
  • Chen L; Merck & Co., Inc., 126 E. Lincoln Ave., Rahway, NJ 07065, USA.
  • Selyutin O; Merck & Co., Inc., 126 E. Lincoln Ave., Rahway, NJ 07065, USA.
  • Zeng Q; Merck & Co., Inc., 126 E. Lincoln Ave., Rahway, NJ 07065, USA.
  • Dwyer MP; Merck & Co., Inc., 126 E. Lincoln Ave., Rahway, NJ 07065, USA.
  • Nair AG; Merck & Co., Inc., 126 E. Lincoln Ave., Rahway, NJ 07065, USA.
  • Shankar BB; Merck & Co., Inc., 126 E. Lincoln Ave., Rahway, NJ 07065, USA.
  • Kim SH; Merck & Co., Inc., 126 E. Lincoln Ave., Rahway, NJ 07065, USA.
  • Yang DY; Merck & Co., Inc., 126 E. Lincoln Ave., Rahway, NJ 07065, USA.
  • Rosenblum SB; Merck & Co., Inc., 126 E. Lincoln Ave., Rahway, NJ 07065, USA.
  • Ruck RT; Merck & Co., Inc., 126 E. Lincoln Ave., Rahway, NJ 07065, USA.
  • Davies IW; Merck & Co., Inc., 126 E. Lincoln Ave., Rahway, NJ 07065, USA.
  • Hu B; Department of Medicinal Chemistry, WuXi AppTec, Shanghai 200131, China.
  • Zhong B; Department of Medicinal Chemistry, WuXi AppTec, Shanghai 200131, China.
  • Hao J; Department of Medicinal Chemistry, WuXi AppTec, Shanghai 200131, China.
  • Ji T; Department of Medicinal Chemistry, WuXi AppTec, Shanghai 200131, China.
  • Zan S; Department of Medicinal Chemistry, WuXi AppTec, Shanghai 200131, China.
  • Liu R; Merck & Co., Inc., 126 E. Lincoln Ave., Rahway, NJ 07065, USA.
  • Agrawal S; Merck & Co., Inc., 126 E. Lincoln Ave., Rahway, NJ 07065, USA.
  • Carr D; Merck & Co., Inc., 126 E. Lincoln Ave., Rahway, NJ 07065, USA.
  • Curry S; Merck & Co., Inc., 126 E. Lincoln Ave., Rahway, NJ 07065, USA.
  • McMonagle P; Merck & Co., Inc., 126 E. Lincoln Ave., Rahway, NJ 07065, USA.
  • Bystol K; Merck & Co., Inc., 126 E. Lincoln Ave., Rahway, NJ 07065, USA.
  • Lahser F; Merck & Co., Inc., 126 E. Lincoln Ave., Rahway, NJ 07065, USA.
  • Ingravallo P; Merck & Co., Inc., 126 E. Lincoln Ave., Rahway, NJ 07065, USA.
  • Chen S; Merck & Co., Inc., 126 E. Lincoln Ave., Rahway, NJ 07065, USA.
  • Asante-Appiah E; Merck & Co., Inc., 126 E. Lincoln Ave., Rahway, NJ 07065, USA.
  • Kozlowski JA; Merck & Co., Inc., 126 E. Lincoln Ave., Rahway, NJ 07065, USA.
Bioorg Med Chem Lett ; 26(21): 5354-5360, 2016 11 01.
Article em En | MEDLINE | ID: mdl-27680588
We describe the impact of proline modifications, in our tetracyclic-indole based series of nonstructural protein 5A (NS5A) inhibitors, to their replicon profiles. This work identified NS5A inhibitors with an improved and flattened resistance profiles.
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Texto completo: 1 Base de dados: MEDLINE Assunto principal: Antivirais / Benzofuranos / Prolina / Proteínas não Estruturais Virais / Imidazóis / Indóis Idioma: En Ano de publicação: 2016 Tipo de documento: Article
Texto completo
Imprimir
XML
PubMed Links
Buscar no Google

Texto completo: 1 Base de dados: MEDLINE Assunto principal: Antivirais / Benzofuranos / Prolina / Proteínas não Estruturais Virais / Imidazóis / Indóis Idioma: En Ano de publicação: 2016 Tipo de documento: Article