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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.

SUBMITTER: Zhou G 

PROVIDER: S-EPMC2833348 | biostudies-literature | 2010 Mar

REPOSITORIES: biostudies-literature

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

Zhou Guangyan G   Wu Dong D   Hermel Evan E   Balogh Edina E   Gochin Miriam M  

Bioorganic & medicinal chemistry letters 20100125 5


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 effecti  ...[more]

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