Effect of the diamine nonleaving group in platinum-acridinylthiourea conjugates on DNA damage and cytotoxicity.
J Med Chem
; 50(9): 2259-63, 2007 May 03.
Article
em En
| MEDLINE
| ID: mdl-17408248
ABSTRACT
The following complexes of type [PtCl(R)(ACRAMTU)](NO3)2 (ACRAMTU = 1-[2-(acridin-9-ylamino)ethyl]-1,3-dimethylthiourea)), derived from prototype 1 (with R = ethane-1,2-diamine), were synthesized 2 (with R = (1R,2R)-1,2-diaminocyclohexane), 3 (with R = propane-1,3-diamine), 4 (with R = N1,N1,N2,N2-tetramethylethane-1,2-diamine), and 5 (with R = 2,2'-bipyridine). The DNA sequence specificity of the conjugates and their antiproliferative potential in HL-60 and H460 cells were investigated. Conjugate 3 showed the strongest non-cisplatin-type DNA damage in polymerase stop assays and superior cell kill efficacy in H460 lung cancer (IC50 = 70 nM).
Buscar no Google
Base de dados:
MEDLINE
Assunto principal:
Compostos Organoplatínicos
/
Tioureia
/
Acridinas
/
Dano ao DNA
/
Antineoplásicos
Limite:
Humans
Idioma:
En
Ano de publicação:
2007
Tipo de documento:
Article