Detail of "147127-19-3"

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Cytostatic activity of antiviral acyclic nucleoside phosphonates in rodent lymphocytes

Cytostatic activity of antiviral acyclic nucleoside phosphonates in rodent lymphocytes. Zidek, Zdenek; Potmesil, Petr; Holy, Antonin (Institute of Experimental Medicine, Academy of Sciences of the Czech Republic, Prague 142 20, Czech Rep.). Toxicology and Applied Pharmacology, 192(3), 246-253 (English) 2003 Elsevier Science. CODEN: TXAPA9. ISSN: 0041-008X. DOCUMENT TYPE: Journal CA Section: 1 (Pharmacology) Acyclic nucleoside phosphonates (ANPs) inhibit replication of both DNA viruses and retroviruses, including HIV. The major mechanism of their antiviral action is inhibition of virus-induced DNA polymerases and/or of reverse transcriptases. We investigated the effects of ANPs on proliferation of mitogen-stimulated mouse and rat splenocytes. Included in the study were compds. differing at the heterocyclic base, i.e., adenine (A) and 2,6-diaminopurine (DAP), and at the N9-side chain, i.e., 9-[2-(phosphonomethoxy)ethyl] (PME) and (R)- or (S)-enantiomers of 9-[2-(phosphonomethoxy)propyl] (PMP) moieties, and their numerous N6-substituted derivs. The medial inhibitory concns. (IC50) of N6-nonsubstituted compds. range from 0.13 (PMEDAP) to 354 mM ((R)-PMPA). Antiproliferative effects are more pronounced in PME than in PMP series, and they are more prominent in DAP compared to A analogs. The (S)-enantiomers of PMP series are more effective than corresponding (R)-congers. The highest cytostatic potential is exhibited by N6-allyl-PMEDAP (IC50=0.017 mM) and N6-cyclopropyl-PMEDAP (IC50=0. 147127-19-3 and 147057-09-8 which are cas registry numbers of substances are two of reagents here.036 mM). The N6-substituted derivs. of (S)-PMPA are virtually devoid of cytostatic activity. No tight correlation between the cytostatic and reported antiviral effects could be detected. .