PMID- 12954073 OWN - NLM STAT- MEDLINE DCOM- 20031110 LR - 20221207 IS - 0022-2623 (Print) IS - 0022-2623 (Linking) VI - 46 IP - 19 DP - 2003 Sep 11 TI - Synthesis and cytotoxic activity of two novel 1-dodecylthio-2-decyloxypropyl-3-phosphatidic acid conjugates with gemcitabine and cytosine arabinoside. PG - 4205-8 AB - 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. FAU - Alexander, Richard L AU - Alexander RL AD - Department of Physiology and Pharmacology, Wake Forest University School of Medicine, Medical Center Boulevard, Winston-Salem, North Carolina 27517, USA. FAU - Morris-Natschke, Susan L AU - Morris-Natschke SL FAU - Ishaq, Khalid S AU - Ishaq KS FAU - Fleming, Ronald A AU - Fleming RA FAU - Kucera, Gregory L AU - Kucera GL LA - eng PT - Comparative Study PT - Journal Article PT - Research Support, Non-U.S. Gov't PL - United States TA - J Med Chem JT - Journal of medicinal chemistry JID - 9716531 RN - 0 (Antineoplastic Agents) RN - 0 (Buffers) RN - 0 (Phosphatidic Acids) RN - 04079A1RDZ (Cytarabine) RN - 0W860991D6 (Deoxycytidine) RN - EC 1.17.4.- (Ribonucleotide Reductases) RN - 0 (Gemcitabine) SB - IM MH - Antineoplastic Agents/chemical synthesis/*chemistry/pharmacokinetics/*pharmacology MH - Buffers MH - Cell Line MH - Cytarabine/*analogs & derivatives/pharmacology MH - Deoxycytidine/*analogs & derivatives/*chemistry/pharmacology MH - Humans MH - Inhibitory Concentration 50 MH - Phosphatidic Acids/chemical synthesis/*chemistry/pharmacokinetics/*pharmacology MH - Ribonucleotide Reductases/antagonists & inhibitors MH - Solubility MH - Gemcitabine EDAT- 2003/09/05 05:00 MHDA- 2003/11/11 05:00 CRDT- 2003/09/05 05:00 PHST- 2003/09/05 05:00 [pubmed] PHST- 2003/11/11 05:00 [medline] PHST- 2003/09/05 05:00 [entrez] AID - 10.1021/jm020571x [doi] PST - ppublish SO - J Med Chem. 2003 Sep 11;46(19):4205-8. doi: 10.1021/jm020571x.