title: Antiproliferative activity and mechanism of action of fatty acid derivatives of arabinosylcytosine (ara-C) in leukemia and solid tumor cell lines.
abstract: Resistance to, the hydrophilic drug ara-C, might be meditated by decreased membrane transport. Lipophilic prodrugs were synthesized to facilitate uptake. These compounds were equally active as ara-C, while the compounds with the shortest fatty-acid group and highest number of double bonds were the more active. These compounds also show a better retention profile, their effect is retained longer than for ara-C.
authors.affiliation: Department of Medical Oncology, VU University Medical Center, Amsterdam, The Netherlands.
authors.forename: A M
authors.initials: AM
authors.lastname: Bergman
authors.forename: C M
authors.initials: CM
authors.lastname: Kuiper
authors.forename: F
authors.initials: F
authors.lastname: Myhren
authors.forename: M L
authors.initials: ML
authors.lastname: Sandvold
authors.forename: H R
authors.initials: HR
authors.lastname: Hendriks
authors.forename: G J
authors.initials: GJ
authors.lastname: Peters
mesh_terms: D000818:Animals; D000964:Antimetabolites, Antineoplastic / Q000494:pharmacology*; D045744:Cell Line, Tumor; D049109:Cell Proliferation / Q000187:drug effects; D003561:Cytarabine / Q000494:pharmacology*; D003841:Deoxycytidine / Q000031:analogs & derivatives* / Q000494:pharmacology; D004305:Dose-Response Relationship, Drug; D019008:Drug Resistance, Neoplasm; D005227:Fatty Acids / Q000378:metabolism*; D006801:Humans; D020128:Inhibitory Concentration 50; D007938:Leukemia / Q000188:drug therapy*; D051379:Mice; D009369:Neoplasms / Q000188:drug therapy*; D051381:Rats; D013997:Time Factors; D000093542:Gemcitabine
chemical_list: D000964:Antimetabolites, Antineoplastic; D005227:Fatty Acids; D003561:Cytarabine; D003841:Deoxycytidine; D000093542:Gemcitabine