Synthesis and antitumor activity of benzoic nitrogen mustard derivatives / 药学学报
Acta Pharmaceutica Sinica
;
(12): 1327-1329, 2007.
Artigo
em Chinês
| WPRIM
| ID: wpr-268182
ABSTRACT
To study the effect of isoprenoid and aliphatic saturated alcohols as modificator on benzoic nitrogen mustard, the intermediate 4-[N,N-bis(2-chloroethyl) amino] benzoic acid 4 was prepared in four steps utilizing p-amino benzoic acid as the starting material. Target compounds were synthesized by the catalytic esterification of DCC/DMAP and the structures of the six new esters were characterized by elemental analysis, 1H NMR, 13C NMR and MS. Antitumor activities were evaluated in vitro using MTT assay. The result showed that some derivatives were more potent than the intermediate 4, and compound 5c modified with dodecanol exhibited similar activity to the commercial drug melphalan.
Texto completo:
DisponíveL
Índice:
WPRIM (Pacífico Ocidental)
Assunto principal:
Patologia
/
Farmacologia
/
Melanoma Experimental
/
Cricetulus
/
Células CHO
/
Antineoplásicos Alquilantes
/
Células K562
/
Concentração Inibidora 50
/
Linhagem Celular Tumoral
/
Proliferação de Células
Limite:
Animais
/
Humanos
Idioma:
Chinês
Revista:
Acta Pharmaceutica Sinica
Ano de publicação:
2007
Tipo de documento:
Artigo
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