SAR and Lead Optimization of an HIV-1 Vif-APOBEC3G Axis Inhibitor.
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ABSTRACT:
SUBMITTER: Mohammed I
PROVIDER: S-EPMC3922209 | biostudies-literature | 2012 Jun
REPOSITORIES: biostudies-literature
Publications
SAR and Lead Optimization of an HIV-1 Vif-APOBEC3G Axis Inhibitor.
Mohammed Idrees I Parai Maloy K MK Jiang Xinpeng X Sharova Natalia N Singh Gatikrushna G Stevenson Mario M Rana Tariq M TM
ACS medicinal chemistry letters 20120601 6
We describe structure-activity relationship and optimization studies of RN-18, an HIV-1 Vif-APOBEC3G axis inhibitor. Targeted modifications of RN-18 ring-C, ring-B, ring-A, bridge A-B, and bridge B-C were performed to identify the crucial structural features, which generated new inhibitors with similar (<b>4g</b> and <b>4i</b>) and improved (<b>5</b>, <b>8b</b>, and <b>11</b>) activities. Two potent water-soluble RN-18 analogues, <b>17</b> and <b>19,</b> are also disclosed, and we describe the r ...[more]
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