Abstract: Synthetic analogs of 2',5'-oligoadenylate wherein the aglycon, ribosyl moiety and/or terminal nucleoside have been modified are effective antiviral agents for pharmaceutical and agricultural use. They are particularly useful in inhibiting replication of tobacco mosaic virus. Novel synthetic analogs have the following formulae wherein m=0, 1, 2 and 3 and n=0, 1, 2, 3 or 4: ##STR1##The invention described herein was supported by National Institutes of Health Grant GM-26134 and National Science Foundation Grant PCM-8111752.

Abstract: The method of making radioiodinated pyrimidine nucleoside or nucleotide which comprises contacting a water-insoluble halomercuri pyrimidine nucleoside or nucleotide with an aqueous medium containing a dissolved radioactive iodide ion and an oxidizing agent, the molar amounts of said nucleoside or nucleotide and said oxidizing agent being in excess of the molar amount of said iodide, whereby water-soluble radioactive iodinated pyrimidine nucleoside or nucleotide is formed in solution, and separating residual water-insoluble halomercuri pyrimidine nucleoside or nucleotide from said solution.

Abstract: Novel medicinal agent for the topical treatment of viral diseases, containing 5-ethyl-2'-deoxyuridine as the antivirally active compound and urea as the penetration-promoting compound, in an aqueous gel.

Abstract: The invention consists of compounds and methods for the synthesis of oligonucleotides which contain one or more free aliphatic amino groups attached to the sugar moieties of the nucleoside subunits. The synthetic method is versatile and general, permitting amino groups to be selectively placed at any position on oligonucleotides of any composition or length which is attainable by current DNA synthetic methods. Fluorescent dyes or other detectable moieties may be covalently attached to the amino groups to yield the corresponding modified oligonucleotide.

Abstract: A carried sheet being formed of a cellulose or a nitrocellulose derivative and coated with polyuridylic acid or polythymidylic acid or a mixture thereof. A method of using the carrier sheet for preparative recovery of mRNA.

Abstract: A compound which exhibits antiviral activity towards HTLV-III/LAV, having the formula: ##STR1## wherein R.sup.4 is O or NH;R.sup.5 is a C.sub.2-4 alkyl group or a C.sub.3-4 cycloalkyl group, whereinsaid alkyl group or cycloalkyl group may be substituted by one or more of Cl, Br, I, F, OH, N.sub.3, NH.sub.2, SO.sub.3 H, or COOH;R.sup.6 is hydrogen or a C.sub.1 -C.sub.4 alkyl group, which may be substituted by Cl, Br, I, F, OH, N.sub.3, NH.sub.2, SO.sub.3 H, or COOH;R.sup.3' is N.sub.3, NH.sub.2, or H; and R.sup.5' is N.sub.3, NH.sub.2, OH, phosphate, or a C.sub.1-4 acyl group.

Abstract: The present invention relates to a chemical compound which consists of an oligonucleotide or an oligodeoxynucleotide consisting of a natural or modified chain of nucleotides (sic) to which an intercalating group is fixed via a covalent bond.

Abstract: Hypocholesterolemically and/or hypotriglyceridemically active RNA fractions having the following characteristics:(a) Molecular weight by gel filtration: 2,000.+-.1,000(b) Base composition ratio of nucleic acid: uracil: guanine: cytosine: adenine=13.0: 16.0: 16.0: 10.0(c) Infrared absorption sepctrum: shown in FIG. 2(d) Physiological characteristics: having a hypocholesterolemic and/or hypotriglyceridemic activity in mammals.These hypocholesterolemically and/or hypotriglyceridemically active RNA fractions can be prepared by cultivating a microorganism belonging to the genus Streptococcus in an adequate culture medium therefor; and collecting the hypocholesterolemically and/or hypotriglyceridemically active RNA fractions from the cultured cells of the microorganism.

Abstract: Nucleotide analogs, modified by the attachment at hydrogen bonding positions of linker groups, that is, the 6-position of adenine, 4-position of cytosine, and 2-position of guanine, are prepared. Such analogs, alone or with reporter groups attached, may be incorporated into DNA probes which effectively hybridize to target DNA.

Abstract: A method for the stereoselective snythesis of a cis-syn, furan-side mono-adducted linear furocoumarin:nucleoside adduct, which comprises reacting a linear furocoumarin with a nucleophilic acid to form a 3,4-dihydro-4-substituted linear furocoumarin intermediate, and contacting the intermediate with a nucleoside under photoactivating conditions. The reaction produces a cis-syn, furan-side, mono-adducted 3,4-dihydro-4-substituted linear furocoumarin:nucleoside adduct which can then be deblocked to give the final product under mild conditions.

Abstract: An oligonucleotide derivative having an amino group protected with an eliminatable group bonded through a phosphate group and a spacer with an appropriate length to the 5'-end of an oligonucleotide protected suitably at the 3'-hydroxyl group and the base moiety of the nucleotide, and an immobilized oligonucleotide derivative having a Sepharose carrier bonded to the amino group in place of said protective group are disclosed. Methods for production of these derivatives are also disclosed.

Abstract: A method is provided for capping failure sequences in oligonucleotide synthesis by phosphitylation. A phosphite monoester is reacted with the 5' or 3' hydroxyl of the failure sequence between successive condensation steps in a synthesis procedure to form a 5' or 3' phosphite diester with the failure sequence. The phosphite diester substituent is inert with respect to subsequent reaction steps in the synthesis of the desired oligonucleotide product.

Abstract: Protective groups are provided which are suitable for masking phosphates and phosphonates. The protected compositions can be introduced in a biological system and then demasked under certain biological conditions. This method permits phosphates and phosphonates which would themselves degrade in the biological system and therefore be ineffective to be introduced in a protected form and late released under the proper conditions.

Abstract: Disclosed herein are a novel process for producing 1-.beta.-D-arabinofuranosylcytosine-5'-stearylphosphate monosodium salt, which has been expected as an oral antitumor agent, and 1-.beta.-D-arabinofranosylcytosine-5'-stearylphosphate monosodium salt monohydrate obtained from the above-mentioned monosodium salt.

Abstract: A compound of the formula ##STR1## wherein R.sub.1 and R.sub.2 are long-chain fatty acid residue, and Ns is nucleoside residue selected from the group consisting of 5-fluorouridine-5'-yl, 5-fluoro-2'-deoxyuridine-5'-yl-, bredinin-5'-yl, tubercidine-5'-yl-, neplanocin A-6'-yl-, 5-fluorocytidine-5'-yl-, arabinosylcytosine-5'-yl, arabinocyl-5-fluorocytosine-5'-yl-, arabinosyladenine-5'-yl- and arabinosylthymine-5 '-yl-, and pharmacologically acceptable salts thereof, having antitumor activity.

Abstract: Sybthesis of new biologically active fluorescent cyclic nucleotides of general formula: ##STR1## wherein X=OH and Y=NH.sub.2 or X=NH.sub.2 and Y=H and L is a fluorescent group of the class of 5 (or 6)-thioacetamido-fluorescein or of 5(or 8)-(2 thioacetamido-ethyl)-amino-naphthalene -1-sulphonic acid.

Abstract: An oligonucleotide derivative having an amino group protected with an eliminatable group bonded through a phosphate group and a spacer with an appropriate length to the 5'-end of an oligonucleotide protected suitably at the 3'-hydroxyl group and the base moiety of the nucleotide, and an immobilized oligonucleotide derivative having a Sepharose carrier bonded to the amino group in place of said protective group are disclosed. Methods for production of these derivatives are also disclosed.

Abstract: 5-substituted 2',3'-dideoxycytidine compounds and their monophosphates are disclosed which have been found to have potent activity against retroviruses. The 5-fluoro-and 5-aza-substituted 2',3'-dideoycytidine compounds have been found to be effective against HTLV-III/LAV virus.

Abstract: Novel biotinylated nucleotides have a chemically cleavable linker arm between a biotin and an organic basic group. They are useful in a method of isolating target macromolecules from crude physiological mixtures. The biotinylated nucleotides are bound via their organic basic groups to macromolecules having an affinity for the target macromolecules and brought into contact with the target macromolecules to form a biotinylated nucleotide-affinity macromolecule - target macromolecule complex. The complex thus obtained is brought into contact with immobilized avidin whereupon the biotin moeity binds to the avidin. The complex and avidin are washed to remove undesired substances and then the chemically cleavable bond in the nucleotide is cleaved to obtain the affinity-macromolecule - target macromolecule complex from which the target macromolecule can be obtained.

Abstract: A method for synthesizing monofluoromethyl- and difluoromethyluracil nucleosides from the corresponding thymine nucleosides is developed. These compounds which contain a partially fluorinated methyl group at the C-5 position (a new class of nucleosides) are potential antiviral and/or anticancer agents. The major features of the preparative route involve bromination of suitably protected thymine nucleosides followed by fluoride treatment.