PT  - JOURNAL ARTICLE
AU  - E De Clercq
AU  - J Balzarini
AU  - J Descamps
AU  - G F Huang
AU  - P F Torrence
AU  - D E Bergstrom
AU  - A S Jones
AU  - P Serafinowski
AU  - G Verhelst
AU  - R T Walker
TI  - Antiviral, antimetabolic, and cytotoxic activities of 5-substituted 2'-deoxycytidines.
DP  - 1982 Jan 01
TA  - Molecular Pharmacology
PG  - 217--223
VI  - 21
IP  - 1
4099  - http://molpharm.aspetjournals.org/content/21/1/217.short
4100  - http://molpharm.aspetjournals.org/content/21/1/217.full
SO  - Mol Pharmacol1982 Jan 01; 21
AB  - Various 5-substituted 2'-deoxycytidines, including 5-bromo-dCyd, 5-iodo-dCyd, 5-nitro-dCyd, 5-ethynyl-dCyd, 5-propyl-dCyd, (E)-5-(2-bromovinyl)-dCyd, and (E)-5-(2-iodovinyl)-dCyd, were evaluated for their antiviral and antimetabolic properties in primary rabbit kidney (PRK) cell cultures and for their inhibitory effects on murine L1210 cell proliferation. All dCyd analogues proved to be selective inhibitors of herpes simplex virus (HSV) replication: 5-bromo-dCyd, 5-iodo-dCyd, 5-nitro-dCyd, and 5-ethynyl-dCyd were more selective in their anti-HSV activity than were the corresponding 5-substituted 2'-deoxyuridines, whereas 5-propyl-dCyd, (E)-5-(2-bromovinyl)-dCyd, and (E)-5-(2-iodovinyl)-dCyd were as selective as their dUrd counterparts. The dCyd analogues were also less cytotoxic (for both PRK and L1210 cells), as could be monitored by inhibition of either cell proliferation or host-cell DNA synthesis (incorporation of radiolabeled precursors). Of all 5-substituted 2'-deoxycytidines tested, the (E)-5-(2-halogenovinyl) derivatives emerged as the most potent and most selective inhibitors of HSV (Type 1) replication.