Synthesis and antitumor activity of benzoic nitrogen mustard derivatives / 药学学报
Acta Pharmaceutica Sinica
;
(12): 1327-1329, 2007.
Article
in Chinese
| 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.
Full text:
Available
Index:
WPRIM (Western Pacific)
Main subject:
Pathology
/
Pharmacology
/
Melanoma, Experimental
/
Cricetulus
/
CHO Cells
/
Antineoplastic Agents, Alkylating
/
K562 Cells
/
Inhibitory Concentration 50
/
Cell Line, Tumor
/
Cell Proliferation
Limits:
Animals
/
Humans
Language:
Chinese
Journal:
Acta Pharmaceutica Sinica
Year:
2007
Type:
Article
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