Phenothiazine-based CaaX competitive inhibitors of human farnesyltransferase bearing a cysteine, methionine, serine or valine moiety as a new family of antitumoral compounds.
Bioorg Med Chem Lett
; 25(20): 4447-52, 2015 Oct 15.
Article
em En
| MEDLINE
| ID: mdl-26372651
ABSTRACT
A new family of CaaX competitive inhibitors of human farnesyltransferase based on phenothiazine and carbazole skeleton bearing a l-cysteine, l-methionine, l-serine or l-valine moiety was designed, synthesized and biologically evaluated. Phenothiazine derivatives proved to be more active than carbazole-based compounds. Phenothiazine 1b with cysteine residue was the most promising inhibitor of human farnesyltransferase in the current study.
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Base de dados:
MEDLINE
Assunto principal:
Fenotiazinas
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Inibidores Enzimáticos
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Farnesiltranstransferase
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Aminoácidos
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Antineoplásicos
Idioma:
En
Ano de publicação:
2015
Tipo de documento:
Article