Benzothiazole-containing hydroxamic acids as histone deacetylase inhibitors and antitumor agents.
Bioorg Med Chem Lett
; 21(24): 7509-12, 2011 Dec 15.
Article
en En
| MEDLINE
| ID: mdl-22036991
ABSTRACT
Data from clinical studies indicate that inhibitors of Class I and Class II histone deacetylase (HDAC) enzymes show great promise for the treatment of cancer. Zolinza (SAHA, Zolinza) was recently approved by the FDA for the treatment of the cutaneous manifestations of cutaneous T-cell lymphoma. As a part of our ongoing effort to identify novel small molecules to target these important enzymes, we have prepared two series of benzothiazole-containing analogues of SAHA. It was found that several compounds with 6C-bridge linking benzothiazole moiety and hydroxamic functional groups showed good inhibition against HDAC3 and 4 at as low as 1 µg/ml and exhibited potent cytotoxicity against five cancer cell lines with average IC(50) values of as low as 0.81 µg/ml, almost equipotent to SAHA.
Texto completo:
1
Colección:
01-internacional
Base de datos:
MEDLINE
Asunto principal:
Benzotiazoles
/
Inhibidores de Histona Desacetilasas
/
Histona Desacetilasas
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Ácidos Hidroxámicos
/
Antineoplásicos
Tipo de estudio:
Prognostic_studies
Límite:
Humans
Idioma:
En
Revista:
Bioorg Med Chem Lett
Asunto de la revista:
BIOQUIMICA
/
QUIMICA
Año:
2011
Tipo del documento:
Article