-transparent.png){kind=logo}
N1-Heterocyclic pyrimidinediones as non-nucleoside inhibitors of HIV-1 reverse transcriptase. 2010
Michael L Mitchell, and
Jong Chan Son, and
Ill Young Lee, and
Chong-Kyo Lee, and
Hae Soo Kim, and
Hongyan Guo, and
Jianhong Wang, and
Jaclyn Hayes, and
Michael Wang, and
Amber Paul, and
Eric B Lansdon, and
James M Chen, and
Gene Eisenberg, and
Romas Geleziunas, and
Lianhong Xu, and
Choung U Kim
Gilead Sciences, Inc., 333 Lakeside Drive, Foster City, CA 94404, USA. mmitchell@gilead.com
A series of N1-heterocyclic pyrimidinediones were extensively evaluated as HIV-1 non-nucleoside reverse transcriptase inhibitors (NNRTIs). Inhibitor 1 is active against NNRTI-resistant viruses including RT mutant K103N. The co-crystal structure of inhibitor 1 with HIV-1 RT revealed that H-bonds are formed with K101 and K103. Efforts to improve the suboptimal pharmacokinetic profile of 1 resulted in the discovery of compound 13, which represents the lead compound in this series with improved pharmacokinetics and similar potency as inhibitor 1.
Related Publications
Michael L Mitchell, and
Jong Chan Son, and
Ill Young Lee, and
Chong-Kyo Lee, and
Hae Soo Kim, and
Hongyan Guo, and
Jianhong Wang, and
Jaclyn Hayes, and
Michael Wang, and
Amber Paul, and
Eric B Lansdon, and
James M Chen, and
Gene Eisenberg, and
Romas Geleziunas, and
Lianhong Xu, and
Choung U Kim
February 2004,
Journal of medicinal chemistry,
Michael L Mitchell, and
Jong Chan Son, and
Ill Young Lee, and
Chong-Kyo Lee, and
Hae Soo Kim, and
Hongyan Guo, and
Jianhong Wang, and
Jaclyn Hayes, and
Michael Wang, and
Amber Paul, and
Eric B Lansdon, and
James M Chen, and
Gene Eisenberg, and
Romas Geleziunas, and
Lianhong Xu, and
Choung U Kim
February 2006,
Current opinion in investigational drugs (London, England : 2000),
Michael L Mitchell, and
Jong Chan Son, and
Ill Young Lee, and
Chong-Kyo Lee, and
Hae Soo Kim, and
Hongyan Guo, and
Jianhong Wang, and
Jaclyn Hayes, and
Michael Wang, and
Amber Paul, and
Eric B Lansdon, and
James M Chen, and
Gene Eisenberg, and
Romas Geleziunas, and
Lianhong Xu, and
Choung U Kim
December 2013,
Future medicinal chemistry,
Michael L Mitchell, and
Jong Chan Son, and
Ill Young Lee, and
Chong-Kyo Lee, and
Hae Soo Kim, and
Hongyan Guo, and
Jianhong Wang, and
Jaclyn Hayes, and
Michael Wang, and
Amber Paul, and
Eric B Lansdon, and
James M Chen, and
Gene Eisenberg, and
Romas Geleziunas, and
Lianhong Xu, and
Choung U Kim
February 2006,
Bioorganic & medicinal chemistry letters,
Michael L Mitchell, and
Jong Chan Son, and
Ill Young Lee, and
Chong-Kyo Lee, and
Hae Soo Kim, and
Hongyan Guo, and
Jianhong Wang, and
Jaclyn Hayes, and
Michael Wang, and
Amber Paul, and
Eric B Lansdon, and
James M Chen, and
Gene Eisenberg, and
Romas Geleziunas, and
Lianhong Xu, and
Choung U Kim
April 2012,
Bioorganic & medicinal chemistry letters,
Michael L Mitchell, and
Jong Chan Son, and
Ill Young Lee, and
Chong-Kyo Lee, and
Hae Soo Kim, and
Hongyan Guo, and
Jianhong Wang, and
Jaclyn Hayes, and
Michael Wang, and
Amber Paul, and
Eric B Lansdon, and
James M Chen, and
Gene Eisenberg, and
Romas Geleziunas, and
Lianhong Xu, and
Choung U Kim
February 2019,
ACS medicinal chemistry letters,
Michael L Mitchell, and
Jong Chan Son, and
Ill Young Lee, and
Chong-Kyo Lee, and
Hae Soo Kim, and
Hongyan Guo, and
Jianhong Wang, and
Jaclyn Hayes, and
Michael Wang, and
Amber Paul, and
Eric B Lansdon, and
James M Chen, and
Gene Eisenberg, and
Romas Geleziunas, and
Lianhong Xu, and
Choung U Kim
February 2017,
Bioorganic chemistry,
Michael L Mitchell, and
Jong Chan Son, and
Ill Young Lee, and
Chong-Kyo Lee, and
Hae Soo Kim, and
Hongyan Guo, and
Jianhong Wang, and
Jaclyn Hayes, and
Michael Wang, and
Amber Paul, and
Eric B Lansdon, and
James M Chen, and
Gene Eisenberg, and
Romas Geleziunas, and
Lianhong Xu, and
Choung U Kim
February 1999,
Drug resistance updates : reviews and commentaries in antimicrobial and anticancer chemotherapy,
Michael L Mitchell, and
Jong Chan Son, and
Ill Young Lee, and
Chong-Kyo Lee, and
Hae Soo Kim, and
Hongyan Guo, and
Jianhong Wang, and
Jaclyn Hayes, and
Michael Wang, and
Amber Paul, and
Eric B Lansdon, and
James M Chen, and
Gene Eisenberg, and
Romas Geleziunas, and
Lianhong Xu, and
Choung U Kim
September 2006,
Bioorganic & medicinal chemistry,
Michael L Mitchell, and
Jong Chan Son, and
Ill Young Lee, and
Chong-Kyo Lee, and
Hae Soo Kim, and
Hongyan Guo, and
Jianhong Wang, and
Jaclyn Hayes, and
Michael Wang, and
Amber Paul, and
Eric B Lansdon, and
James M Chen, and
Gene Eisenberg, and
Romas Geleziunas, and
Lianhong Xu, and
Choung U Kim
June 2003,
AIDS (London, England),
