Nichols, D.B. et al. (2012) Inhibition of hepatitis C virus NS5B polymerase by S-trityl-l-cysteine derivatives. European Journal of Medicinal Chemistry, 49, pp. 191-199. (doi: 10.1016/j.ejmech.2012.01.010)
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Abstract
Structure-based studies led to the identification of a constrained derivative of S-trityl-l-cysteine (STLC) scaffold as a candidate inhibitor of hepatitis C virus (HCV) NS5B polymerase. A panel of STLC derivatives were synthesized and investigated for their activity against HCV NS5B. Three STLC derivatives, 9, F-3070, and F-3065, were identified as modest HCV NS5B inhibitors with IC50 values between 22.3 and 39.7 μM. F-3070 and F-3065 displayed potent inhibition of intracellular NS5B activity in the BHK-NS5B-FRLuc reporter and also inhibited HCV RNA replication in the Huh7/Rep-Feo1b reporter system. Binding mode investigations suggested that the STLC scaffold can be used to develop new NS5B inhibitors by further chemical modification at one of the trityl phenyl group.
| Item Type: | Articles |
|---|---|
| Status: | Published |
| Refereed: | Yes |
| Glasgow Author(s) Enlighten ID: | Kozielski, Professor Frank |
| Authors: | Nichols, D.B., Fournet, G., Gurukumar, K.R., Basu, A., Lee, J.-C., Sakamoto, N., Kozielski, F., Musmuca, I., Joseph, B., Ragno, R., and Kaushik-Basu, N. |
| College/School: | College of Medical Veterinary and Life Sciences > School of Cancer Sciences |
| Journal Name: | European Journal of Medicinal Chemistry |
| ISSN: | 0223-5234 |
| Published Online: | 12 January 2012 |
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