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Design, synthesis, and evaluation of indole compounds as novel inhibitors targeting Gp41.

Abstract：

: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 2.1microM, and the IC(50) for cell-cell fusion inhibition was 1.1microM. Assay data indicated that 7 is a promising lead compound for optimization into an effective low molecular weight fusion inhibitor.

journal_name

Bioorg Med Chem Lett

journal_title

Bioorganic & medicinal chemistry letters

authors

Zhou G,Wu D,Hermel E,Balogh E,Gochin M

doi

10.1016/j.bmcl.2010.01.111

subject

Has Abstract

pub_date

2010-03-01 00:00:00

pages

1500-3

issue

5

eissn

0960-894X

issn

1464-3405

pii

S0960-894X(10)00123-X

journal_volume

20

pub_type

杂志文章

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