Synthesis and biological evaluation of water-soluble derivatives of chiral gossypol as HIV fusion inhibitors targeting gp41.
Bioorg Med Chem Lett
; 28(1): 49-52, 2018 01 01.
Article
em En
| MEDLINE
| ID: mdl-29162455
ABSTRACT
A series of novel or known water-soluble derivatives of chiral gossypol were synthesized and screened in vitro for their anti-HIV-1 activity. (-)-gossypol derivative was more active against HIV-1 than the corresponding (+)-gossypol derivative, respectively. Among these derivatives, d-glucosamine derivative of (-)-gossypol, oligopeptide derivative of (-)-gossypol and taurine derivative of (-)-gossypol, such as compounds 1a, 3a and 14a, showed significant inhibitory activities against HIV-1 replication, HIV-1 mediated cell-cell fusion and HIV gp41 6-helix bundle formation as some amino acid derivatives of (-)-gossypol.
Palavras-chave
Texto completo:
1
Base de dados:
MEDLINE
Assunto principal:
Gossipol
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Proteína gp41 do Envelope de HIV
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HIV-1
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Inibidores da Fusão de HIV
Limite:
Humans
Idioma:
En
Ano de publicação:
2018
Tipo de documento:
Article