8-Aza-analogues of PMEA and PMEG: Synthesis and in vitro anti-HIV activity

Article abstract of DOI:10.1080/15257779408009475

8-Aza-analogues of the potent antiviral nucleotide analogues 9-[2- (phosphonomethoxy)ethyl]adenine (PMEA) and 9-[2- (phosphonomethoxy)ethyl]guanine (PMEG) were prepared and evaluated for activity against human immunodeficiency viruses. When compared to the parent compounds, 8-aza-PMEA (1) and -PMEG (2) were less cytotoxic for MT-4 cells, but also less potent against HIV-1 and HIV-2. A new synthesis of PMEG starting from guanine is also reported.

Full text of DOI:10.1080/15257779408009475

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Nucleosides and Nucleotides
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8-Aza-analogues of PMEA and PMEG:
Synthesis and In Vitro Anti-HIV Activity
P. Franchetti a , G. Abu Sheikha a , L. Cappellacci a , L. Messini a , M.
Grifantini a , A. G. Loi b , A. De Montis b , M. G. Spiga b & P. La Colla
b
a Dipartimento di Scienze Chimiche , Università di Camerino , 62032,
Camerino
b Dipartimento di Biologia Sperimentale , Università di Cagliari ,
09124, Cagliari, Italy
Published online: 24 Sep 2006.
To cite this article: P. Franchetti , G. Abu Sheikha , L. Cappellacci , L. Messini , M. Grifantini ,
A. G. Loi , A. De Montis , M. G. Spiga & P. La Colla (1994) 8-Aza-analogues of PMEA and PMEG:
Synthesis and In Vitro Anti-HIV Activity, Nucleosides and Nucleotides, 13:8, 1707-1719, DOI:
10.1080/15257779408009475
To link to this article: http://dx.doi.org/10.1080/15257779408009475
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