Effect of linkage geometry on biological activity in thiourea- and guanidine-substituted acridines and platinum-acridines.
Bioorg Med Chem Lett
; 18(13): 3799-801, 2008 Jul 01.
Article
em En
| MEDLINE
| ID: mdl-18515101
ABSTRACT
Novel thiourea- and guanidine-modified acridine-4-carboxamides (4, 7) and a corresponding platinum-intercalator conjugate (4') have been synthesized and evaluated as cytotoxic agents in human promyelocytic leukemia, HL-60, and a non-small cell lung cancer, NCI-H460. Modification of thiourea sulfur in derivative 4 with a DNA platinating moiety, giving 4', resulted in a pronounced cytotoxic enhancement, and the conjugate proved to be the most active of the newly synthesized compounds in NCI-H460 cells. Conjugate 4' represents a new chemotype with potential applications in the treatment of chemoresistant tumors.
Texto completo:
1
Base de dados:
MEDLINE
Assunto principal:
Platina
/
Tioureia
/
Ureia
/
Acridinas
/
Guanidina
/
Antineoplásicos
Idioma:
En
Ano de publicação:
2008
Tipo de documento:
Article