title: [Acyclic nucleoside phosphonates as potential antineoplastic agents].
abstract: Recently, Gilead Sciences (Foster City, CA, USA) presented a potential cytostatic drug GS-9219. It is a novel lipophilic prodrug of cyprPMEDAP, in vivo releasing the active compound PMEG in a two-step process. GS-9219 has shown a substantial therapeutic potential in treatment of spontaneous non-Hodgkin's lymphoma in dogs and its utilization in the human medicine is prospective. Hence, cyprPMEDAP represents a key intermediate in the intracellular activation of GS-9219. Both acyclic nucleoside phosphonates PMEG and cyprPMEDAP, serving as the basis for development of GS-9219, were discovered and their mechanism of action was investigated in detail at the Institute of Organic Chemistry and Biochemistry, Academy of Sciences of the Czech Republic. The biological studies using the rat lymphoma were carried out at the First Faculty of Medicine, Charles University.
authors.affiliation: Ustav organické chemie a biochemie, v.v.i., AV CR, Praha. votruba@uochb.cas.cz
authors.forename: I
authors.initials: I
authors.lastname: Votruba
authors.forename: B
authors.initials: B
authors.lastname: Otová
authors.forename: A
authors.initials: A
authors.lastname: Holý
mesh_terms: D000225:Adenine / Q000031:analogs & derivatives / Q000494:pharmacology / Q000627:therapeutic use; D000409:Alanine / Q000031:analogs & derivatives / Q000494:pharmacology / Q000627:therapeutic use; D000818:Animals; D000970:Antineoplastic Agents / Q000494:pharmacology / Q000627:therapeutic use; D045744:Cell Line, Tumor / Q000187:drug effects; D006147:Guanine / Q000031:analogs & derivatives / Q000494:pharmacology / Q000627:therapeutic use; D006801:Humans; D008228:Lymphoma, Non-Hodgkin / Q000188:drug therapy; D009705:Nucleosides / Q000494:pharmacology / Q000627:therapeutic use; D063065:Organophosphonates / Q000494:pharmacology / Q000627:therapeutic use; D009943:Organophosphorus Compounds / Q000494:pharmacology / Q000627:therapeutic use; D011687:Purines / Q000494:pharmacology / Q000627:therapeutic use
chemical_list: D000970:Antineoplastic Agents; D009705:Nucleosides; D063065:Organophosphonates; D009943:Organophosphorus Compounds; D011687:Purines; C531423:rabacfosadine; C063380:9-((2-phosphonylmethoxy)ethyl)guanine; C059499:9-(2-phosphonylmethoxyethyl)-2,6-diaminopurine; D006147:Guanine; D000225:Adenine; D000409:Alanine