科研之友
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摘要
A series of indole ring containing compounds were designed based on the structure of the gp41 complex in the region of the hydrophobic pocket. These compounds were synthesized using a Suzuki Coupling reaction, and evaluated using a fluorescence binding assay and cell-cell fusion assay. The observed inhibition constant of compound 7 was 2.1 mu M, and the IC(50) for cell-cell fusion inhibition was 1.1 mu M. Assay data indicated that 7 is a promising lead compound for optimization into an effective low molecular weight fusion inhibitor.
- 出版日期2010-3-1
