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N-alkylated cyclen cobalt(III) complexes of 1-(chloromethyl)-3-(5,6,7-trimethoxyindol-2-ylcarbonyl)-2,3-dihydro-1H-pyrrolo[3,2-f]quinolin-5-ol DNA alkylating agent as hypoxia-activated prodrugs.
Lu, Guo-Liang; Stevenson, Ralph J; Chang, John Yu-Chih; Brothers, Penelope J; Ware, David C; Wilson, William R; Denny, William A; Tercel, Moana.
Afiliação
  • Lu GL; Auckland Cancer Society Research Centre, The University of Auckland, Private Bag 92019, Auckland 1142, New Zealand.
Bioorg Med Chem ; 19(16): 4861-7, 2011 Aug 15.
Article em En | MEDLINE | ID: mdl-21775153
A series of cobalt complexes of the potent DNA minor groove alkylator 1-(chloromethyl)-3-(5,6,7-trimethoxyindol-2-ylcarbonyl)-2,3-dihydro-1H-pyrrolo[3,2-f]quinolin-5-ol (seco-6-azaCBI-TMI) were prepared from a series of N-substituted cyclen ligands. The final N-substituted complexes carried formal overall charges ranging from +2 to -2 and showed limited improvements in solubility. They showed similar stabilities to that of the complex with the unsubstituted cyclen ligand, and large but variable attenuation of the cytotoxicity of the free alkylator (2-30-fold), compared to 150-fold for the unsubstituted ligand. However, they had oxic/hypoxic ratios (2-22-fold) comparable to that of the unsubstituted cyclen complex (5).
Assuntos

Texto completo: 1 Bases de dados: MEDLINE Assunto principal: Pró-Fármacos / Antineoplásicos Alquilantes Limite: Female / Humans Idioma: En Revista: Bioorg Med Chem Assunto da revista: BIOQUIMICA / QUIMICA Ano de publicação: 2011 Tipo de documento: Article País de afiliação: Nova Zelândia

Texto completo: 1 Bases de dados: MEDLINE Assunto principal: Pró-Fármacos / Antineoplásicos Alquilantes Limite: Female / Humans Idioma: En Revista: Bioorg Med Chem Assunto da revista: BIOQUIMICA / QUIMICA Ano de publicação: 2011 Tipo de documento: Article País de afiliação: Nova Zelândia