1,2-Benzisothiazole Derivatives Bearing 4-, 5-, or 6-Alkyl/arylcarboxamide Moieties Inhibit Carbonic Anhydrase Isoform IX (CAIX) and Cell Proliferation under Hypoxic Conditions.
J Med Chem
; 59(13): 6547-52, 2016 07 14.
Article
em En
| MEDLINE
| ID: mdl-27305384
ABSTRACT
Three novel series of 1,2-benzisothiazole derivatives have been developed as inhibitors of carbonic anhydrase isoform IX. Compounds 5c and 5j, tested in vitro on the human colon cell line HT-29, blocked the growth of cells cultured under chemically induced hypoxic conditions, displaying a specific activity against cancer cells characterized by CAIX up-regulation. Moreover, a synergistic activity of 5c with SN-38 (the active metabolite of irinotecan) and 5-fluorouracil on cell proliferation under hypoxic conditions was demonstrated.
Texto completo:
1
Base de dados:
MEDLINE
Assunto principal:
Tiazóis
/
Inibidores da Anidrase Carbônica
/
Anidrase Carbônica IX
/
Antineoplásicos
Limite:
Humans
Idioma:
En
Ano de publicação:
2016
Tipo de documento:
Article