Lipoamino acid conjugates of methotrexate with antitumor activity

被引：21
|
作者：
Pignatello, R
Jansen, G
Kathmann, I
Puglisi, G
Toth, I
机构：
[1] Univ London, Sch Pharm, Dept Pharmaceut & Biol Chem, London WC1N 1AX, England
[2] Univ Hosp Vrije, Dept Oncol, NL-1077 MB Amsterdam, Netherlands
[3] Univ Catania, Dipartimento Sci Farmaceut, I-95125 Catania, Italy
来源：
JOURNAL OF PHARMACEUTICAL SCIENCES | 1998年 / 87卷 / 03期
基金：
英国惠康基金;
关键词：
D O I：
10.1021/js970194p
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
The synthesis, characterization, and in vitro antitumor activity against a wild and a transport-resistant CCRF-CEM cell line is described for a series of alpha,gamma-bisamide lipoamino acid and oligomer conjugates of methotrexate. The influence of the lipophilicity of the conjugates on the cytotoxicity and the dihydrofolate reductase inhibition was investigated. All compounds were more active than their fatty acid conjugate analogues. Compound 1e with a 12-carbon atom aliphatic side chain showed the highest in vitro activity.
引用
收藏
页码：367 / 371
页数：5
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