Synthesis and cytotoxic activity of two novel 1-dodecylthio-2-decyloxypropyl-3-phosphatidic acid conjugates with gemcitabine and cytosine arabinoside

被引：33

作者：

Alexander, RL

Morris-Natschke, SL

Ishaq, KS

Fleming, RA

Kucera, GL

机构：

[1] Wake Forest Univ, Sch Med, Dept Internal Med, Hematol Oncol Sect, Winston Salem, NC 27517 USA

[2] Wake Forest Univ, Sch Med, Dept Physiol & Pharmacol, Winston Salem, NC 27517 USA

[3] Univ N Carolina, Sch Pharm, Dept Med Chem & Nat Prod, Chapel Hill, NC 27599 USA

[4] Kucera Pharmaceut Co, Winston Salem, NC 27101 USA

来源：

JOURNAL OF MEDICINAL CHEMISTRY | 2003年 / 46卷 / 19期

关键词：

D O I：

10.1021/jm020571x

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Cytosine arabinoside (ara-C) and gemcitabine (dFdC) are two standard chemotherapy drugs used in the treatment of patients with various cancers. To alter the pharmacokinetic and pharmacodynamic properties of these molecules, we conjugated a synthetic phospholipid to both ara-C and dFdC and investigated their chemotherapeutic potential. The dFdC conjugate had greater cytotoxic activity compared with the ara-C conjugate and demonstrated notable cytotoxicity against all human cell lines tested.

引用

页码：4205 / 4208

页数：4

共 19 条

[1] KINETIC-STUDIES ON 2',2'-DIFLUORODEOXYCYTIDINE (GEMCITABINE) WITH PURIFIED HUMAN DEOXYCYTIDINE KINASE AND CYTIDINE DEAMINASE [J].