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Bulletin of the Korean Chemical Society (BKCS)

ISSN 0253-2964(Print)
ISSN 1229-5949(Online)
Volume 33, Number 8
BKCSDE 33(8)
August 20, 2012 

Synthesis and Conformation of Novel 3'-Branched Threosyl-5'-Deoxyphosphonic Acid Nucleoside Analogues
Guang Huan Shen, Lien Kang, Eunae Kim, Wonjae Lee, Joon Hee Hong*
Antiviral agent, Threosyl nucleoside phosphonic acid, Conformation analysis
The discovery that threosyl phosphonate nucleoside (PMDTA, EC50 = 2.53 μM) is a potent anti-HIV agent has led to the synthesis and biological evaluation of 5'-deoxy versions of threosyl phosphonate nucleosides. In the present study, (E)-3'-phosphonoalkenyl and 3'-phosphonoalkyl nucleoside analogues 13, 16, 20 and 23 were synthesized from acetol and tested for anti-HIV activity and cytotoxicity. The adenine analogue 16 was found to exhibit moderate in vitro anti-HIV-1 activity (EC50 = 22.2 μM).
2574 - 2580
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