• Archives of Pharmacal Research
• /
• v.12 no.4
• /
• pp.300-305
• /
• 1989

The synthetic study of 3' azido and 3'-fluoro secouridines toward development of new antiviral agents is described. These acyclic nucleosides were synthesized from uridine by the method of ring opening reaction of sugar moiety.

• YAKHAK HOEJI
• /
• v.33 no.5
• /
• pp.296-299
• /
• 1989

The synthetic study of 2', 3'-diazido and difluoro secouridines toward development of new antiviral agents is discribed. These acyclic nucleosides were synthesized from uridine by the method of ring opening reaction of sugar moiety.

• Archives of Pharmacal Research
• /
• v.19 no.1
• /
• pp.62-65
• /
• 1996

A homologous series of twenty, hitherto unreported, analogues of 5-halosubstituted $1, 3-Bis(\omega-cyanoalkyl)uracil$acyclic nucleosides were synthesized by the series of alkylation reactions of 5-halouracils with the corresponding chloroacetonitrile, chloropropionitrile, chlorobutyronitrile and 5-chlorovaleronitrile $(Cl-(C_ 2)_n-CN: n=l, 2, 3, 4)\; in\; anhydrous\; DMSO\; (or DMF)/K_2CO_3(or NaH)\; under\; 75^{\circ}C$ temperature. Antitumor activities for the synthesized compounds were determined against three cell lines (FM-3A cell, P-388 cell and U-938 cell lines). The compounds that exhibited moderate activity to significant activity, included la-b, 2a-b, 3a-c, and 4a, whose compounds were active against P-388, FM-3A and U-937 cell lines with the compounds la, lb, and 2a, showing significant antitumor activity (inhibitory concentrations $(IC_{50})$ ranged from 2.2 to $7.0\mug/ml$). Their strucrure-activity relationship did not show any activity differences in their effective chain length (methyl, ethyl, propyl, butyl) in 1, 3-bis(.omega.-cyanoalkyl) uracils.

• YAKHAK HOEJI
• /
• v.36 no.6
• /
• pp.604-610
• /
• 1992

Synthesis of 6-aza-2´-azido-2´,3´-secouridine, 6-aza-2´,3´-diazido-2´, 3´-secouridine, and 6-aza-5´-azido-2´,3´-secouridine as potential antiviral agents is described. These acyclic nucleosides were synthesized from uridine by the method of ring opening reaction of sugar moiety. And these compounds were tested against HSV-1 and HSV-2, but the in vitro test results of these compounds were negative.

• Bulletin of the Korean Chemical Society
• /
• v.31 no.11
• /
• pp.3348-3352
• /
• 2010

Novel 4'-ethyl-5'-norcarbocyclic adenosine phosphonic acid analogues were synthesized from propionaldehyde 5 through a de novo acyclic synthetic route using reiterative Grignard additions and ring-closing metathesis (RCM) as key reactions. The synthesized nucleoside phosphonic acids analogues 17, 18, 19, and 21 were subjected to antiviral screening against human immunodeficiency virus.