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Tricyclic benzimidazoles as potent poly(ADP-ribose) polymerase-1 inhibitors.
Skalitzky, Donald J; Marakovits, Joseph T; Maegley, Karen A; Ekker, Anne; Yu, Xiao-Hong; Hostomsky, Zdenek; Webber, Stephen E; Eastman, Brian W; Almassy, Robert; Li, Jianke; Curtin, Nicola J; Newell, David R; Calvert, A Hilary; Griffin, Roger J; Golding, Bernard T.
Afiliação
  • Skalitzky DJ; Pfizer Global R&D, La Jolla/Agouron Pharmaceuticals, Inc., San Diego, California 92121, USA.
J Med Chem ; 46(2): 210-3, 2003 Jan 16.
Article em En | MEDLINE | ID: mdl-12519059
ABSTRACT
Novel tricyclic benzimidazole carboxamide poly(ADP-ribose) polymerase-1 (PARP-1) inhibitors have been synthesized. Several compounds were found to be powerful chemopotentiators of temozolomide and topotecan in both A549 and LoVo cell lines. In vitro inhibition of PARP-1 was confirmed by direct measurement of NAD+ depletion and ADP-ribose polymer formation caused by chemically induced DNA damage.
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Base de dados: MEDLINE Assunto principal: Benzimidazóis / Dacarbazina / Inibidores Enzimáticos / Inibidores de Poli(ADP-Ribose) Polimerases / Compostos Heterocíclicos com 3 Anéis Idioma: En Ano de publicação: 2003 Tipo de documento: Article
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PubMed Links

Base de dados: MEDLINE Assunto principal: Benzimidazóis / Dacarbazina / Inibidores Enzimáticos / Inibidores de Poli(ADP-Ribose) Polimerases / Compostos Heterocíclicos com 3 Anéis Idioma: En Ano de publicação: 2003 Tipo de documento: Article