[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: I Votruba, B Otová, A Holý
• Journal: Casopis lekaru ceskych (Cas Lek Cesk) Vol. 147 Issue 9 Pg. 471-7 ( 2008) ISSN: 0008-7335 [Print] Czech Republic
• Vernacular Title: Acyklické nukleosidfosfonáty jako potenciální antineoplastika.
• PMID: 18988489 (Publication Type: Journal Article, Review)

Chemical References

• Antineoplastic Agents
• Nucleosides
• Organophosphonates
• Organophosphorus Compounds
• Purines
• rabacfosadine
• 9-((2-phosphonylmethoxy)ethyl)guanine
• 9-(2-phosphonylmethoxyethyl)-2,6-diaminopurine
• Guanine
• Adenine
• Alanine

Topics

• Adenine (analogs & derivatives, pharmacology, therapeutic use)
• Alanine (analogs & derivatives, pharmacology, therapeutic use)
• Animals
• Antineoplastic Agents (pharmacology, therapeutic use)
• Cell Line, Tumor (drug effects)
• Guanine (analogs & derivatives, pharmacology, therapeutic use)
• Humans
• Lymphoma, Non-Hodgkin (drug therapy)
• Nucleosides (pharmacology, therapeutic use)
• Organophosphonates (pharmacology, therapeutic use)
• Organophosphorus Compounds (pharmacology, therapeutic use)
• Purines (pharmacology, therapeutic use)