1.
Bioorg Med Chem Lett
; 18(8): 2594-8, 2008 Apr 15.
Artículo
en Inglés
| MEDLINE
| ID: mdl-18378445
RESUMEN
The synthesis of new benzimidazole linked pyrrolobenzodiazepine conjugates is described. Some of these conjugates show significant DNA-binding affinity and, a representative compound 4c shows promising in vitro cytotoxicity against a number of human cancer cell lines.
Asunto(s)
Bencimidazoles/química , Benzodiazepinas/síntesis química , Benzodiazepinas/toxicidad , ADN/química , Pirroles/síntesis química , Pirroles/toxicidad , Animales , Benzodiazepinas/química , Bovinos , Línea Celular Tumoral , Supervivencia Celular/efectos de los fármacos , Humanos , Estructura Molecular , Desnaturalización de Ácido Nucleico , Pirroles/química , Relación Estructura-Actividad , Temperatura
2.
Bioorg Med Chem
; 16(7): 3895-906, 2008 Apr 01.
Artículo
en Inglés
| MEDLINE
| ID: mdl-18262426
RESUMEN
Pyrrolobenzodiazepine-diethylphosphonate conjugates have been designed and synthesized that link through two different types of spacers that are simple alkane chain and also a piperazine moiety side-armed with the alkane chains. These pyrrolobenzodiazepine conjugates have exhibited remarkable DNA-binding affinity and improved solubility in water, a representative compound 7d showing promising in vitro cytotoxicity.