Disclosed are halogenated 2-deoxy-lactone, 2′-deoxy-nucleosides, and derivatives thereof, for example, a compound of formula (I). Also disclosed are a composition comprising a pharmaceutically acceptable carrier and at least one compound or salt of the invention, and a method of treating a disorder is selected from the group consisting of an abnormal cellular proliferation, a viral infection, and an autoimmune disorder. ##STR00001##

The invention relates to bola-amphiphilic compounds and their uses for biomedical application. The invention particularly relates to the use of bola-amphiphilic compounds for providing low molecular weight gels (LMWG), useful, in particular, as culture media for animal or human cells, or as biocompatible material for biomedical applications.

Provided are a multi-fluorous blockmer using a readily available fluorous tag and capable of reducing burdens of purification, and an oligonucleotide synthesis method using the same. A multi-fluorous blockmer represented by the formula is synthesized: wherein B is a natural or modified nucleobase; R.sup.1 is a protecting group that can be removed for deprotection under acidic or neutral conditions; R.sup.3 is a protecting group for phosphate; Pro is unprotected, protected, or F-protector, wherein F-protector is O(CH.sub.2).sub.n(CF.sub.2).sub.mCF.sub.3 when the protected moiety of nucleoside base B is O, and is NH(C═O) (CH.sub.2).sub.n(CF.sub.2).sub.mCF.sub.3 when the protected moiety of nucleoside base B is N, wherein n is 1 or 2 and m is an integer of 1 to 20; X is O or S; l is an integer of 0 to 58; R.sup.7 is (C═O) (CH.sub.2).sub.2(C═O) (CH.sub.2).sub.n(CF.sub.2).sub.mCF.sub.3 or a silyl protecting group, wherein n is 1 or 2 and m is an integer of 1 to 20.

##STR00001##

The present application provides compositions and methods for preparing and using “heavy” nucleotide derivatives of thymidine or uridine by replacing the oxygen atom attached to one or more of positions with non-radioactive oxygen-18 (.sup.18O), administering it to a subject to target a tumor including incorporation into tumor cell DNA, and then treating the tumor with proton beam therapy to transmutate the .sup.18O to .sup.18F, resulting in a break of the new fluorine-phosphorous bond. This chemical event destabilizes ribose-phosphate DNA back-bone and base pairing thus produce single- and double strand breaks, clusters lesions that can lead to irreparable DNA damage and enhanced tumor cell killing. The atomic, chemical, and physical aspects result in the use of lower radiation doses and significantly alter acute and late morbidity of radiotherapy. Heavy thymidine and heavy uridine derivatives labeled with .sup.18O have been made and tested.

The present application provides compositions and methods for preparing and using “heavy” nucleotide derivatives of thymidine or uridine by replacing the oxygen atom attached to one or more of positions with non-radioactive oxygen-18 (.sup.18O), administering it to a subject to target a tumor including incorporation into tumor cell DNA, and then treating the tumor with proton beam therapy to transmutate the .sup.18O to .sup.18F, resulting in a break of the new fluorine-phosphorous bond. This chemical event destabilizes ribose-phosphate DNA back-bone and base pairing thus produce single- and double strand breaks, clusters lesions that can lead to irreparable DNA damage and enhanced tumor cell killing. The atomic, chemical, and physical aspects result in the use of lower radiation doses and significantly alter acute and late morbidity of radiotherapy. Heavy thymidine and heavy uridine derivatives labeled with .sup.18O have been made and tested.

Embodiments of the present disclosure relate to nucleotide and nucleoside molecules with acetal 3′-OH blocking groups. Also provided herein are methods to prepare such nucleotide and nucleoside molecules, and the uses of fully functionalized nucleotides containing the 3′ acetal blocking group for sequencing applications.

Embodiments of the present disclosure relate to nucleotide and nucleoside molecules with acetal 3′-OH blocking groups. Also provided herein are methods to prepare such nucleotide and nucleoside molecules, and the uses of fully functionalized nucleotides containing the 3′ acetal blocking group for sequencing applications.

Compositions and methods for preparing and identifying aptamers and aptamer-protein conjugates are provided. The use of a nucleotide analog functionalized with an amine-reactive cross-linker facilitates covalent cross-linking of the aptamer to a protein, in particular site-specific cross-linking to the Fc domain of an antibody.

A nucleoside derivative represented below, or a salt thereof.

##STR00001##

(In (1), R.sup.1 represents a hydrogen atom, a hydroxyl group or a protected group, and in (2), X represent a halogen atom. In (1) and (2), R.sup.2 and R.sup.4 each represent a hydrogen atom, a hydroxyl protecting, phosphate, or protected phosphate group, or —P(═O).sub.nR.sup.5R.sup.6 (n is 0 or 1, R.sup.5 and R.sup.6 each representing a hydrogen atom, hydroxyl, protected hydroxyl, mercapto, protected mercapto, lower alkoxy, cyano lower alkoxy, amino or substituted amino group, when n is 1, R.sup.5 and R.sup.6 are not both hydrogen atoms), R.sup.3 represents NHR.sup.7 (R.sup.7 represents a hydrogen atom, alkyl, alkenyl or protecting group for an amino group), an azide, amidino or guanidino group, each having a linking group (when R.sup.7 is hydrogen atom, the linking group is an alkylene group), and B represents any of a purine-9-yl, 2-oxo-pyrimidin-1-yl, substituted purine-9-yl or substituted 2-oxo-pyrimidin-1-yl group.)

Disclosed herein are derivatives of nucleobase analogues. The disclosed compounds have a nucleobase moiety and an omega-3 polyunsaturated fatty acid moiety, including pharmaceutically acceptable salt or prodrug thereof. Methods of using these compounds for the treatment of cancers such as pancreatic cancer are also disclosed.