Described herein is an enzyme-mediated approach to bioconjugation at nanoparticle (NP) surfaces. This process is enabled by a new synthetic linker compatible with the covalent attachment of alkyne modified substrates, including dyes, peptides and nucleic acids. The methods described herein specifically allow for the linkage of molecules to a DNA-functionalized nanoparticle surface. Enzymatic ligation of molecules to the terminal hydroxyl group of DNA using T4 DNA ligase is achieved through incorporation of a single monophosphate on the approaching substrate. In contrast to previous strategies, the linkers disclosed herein are compatible with alkyne modified molecules of a variety of sizes and charges indicating that the ligase minimally requires the monophosphate and the incoming hydroxyl for conjugation to be successful.

The invention provides novel compounds that may serve as anticancer therapeutics. The compounds of the invention bind to polo-like kinases through the polo-box domain. In certain embodiments, the compounds of the invention are POM-protected peptide derivatives. The use of cationic bis-alkyl his residues in combination with a mono POM-protected phophoryl group results in a peptide possessing an overall neutral charge. The peptide derivatives of the invention have achieved both good efficacy and an enhanced bioavailability. The invention also provides methods of use, compositions, and kits thereof. Further, the invention provides a novel method of design and/or synthesis of phosphoryl-derived peptide derivatives useful as therapeutic agents.

The present invention relates to novel hardeners for curing epoxy resins and to cure accelerants for the accelerated curing of epoxy resins comprising, in each case, at least one compound from the group of esters of phosphorus-containing acids according to Formula (I), wherein there applies to Formula (I):

##STR00001##

wherein there applies to the radicals R.sup.1, R.sup.2, R.sup.3, R.sup.6, X and indices m, n, p, simultaneously or independently of one another: R.sup.1, R.sup.2=simultaneously or independently of one another, hydrogen or alkyl, R.sup.3=alkyl, aryl, O-alkyl, O-aryl, O-alkylaryl or O-arylalkyl, R.sup.6=hydrogen, alkyl or NHC(O)NR.sup.1R.sup.2, X=oxygen or sulphur, m=1, 2 or 3, n=0, 1 or 2, wherein there applies: m+n=3 p=0, 1 or 2.

Provided is a method for producing a vinylphosphonic acid monoester from vinylphosphonic acid diester with high selectivity.

The method for producing a vinylphosphonic acid monoester from a vinylphosphonic acid diester represented by the following Formula (1):

##STR00001##

wherein R.sup.1 and R.sup.2 each independently denote a linear or branched alkyl group having from 1 to 4 carbon atoms, the vinylphosphonic acid monoester being represented by the following Formula (2):

##STR00002##

wherein R.sup.1 denotes a linear or branched alkyl group having from 1 to 4 carbon atoms, according to the invention, wherein the method includes a step of heating the vinylphosphonic acid diester in the presence of a solvent and a basic substance, thereby obtaining the vinylphosphonic acid monoester, and a molar ratio of the basic substance to the vinylphosphonic acid diester is from 0.7 to 3.5.

The invention provides compounds that inhibit cholinesterases, such as acetylcholinesterase and butyrylcholinesterase. Such compounds are useful to prevent or treat exposure of a patient (e.g., a human) to an organophosphoric nerve agent (e.g., sarin and VX) or to treat a patient suffering from a neurodegenerative disorder such as Alzheimer's Disease or Lewy Body Dementia. The compounds are further useful as diagnostic tools for use in medical or research radiography (e.g., positron emission tomography) when synthesized with a radionuclide (e.g., [18F]. Synthetic schemes to produce such compounds are also provided.

The present invention relates to a novel halo-(3-(phenylsulfonyl)prop-1-enyl)pyridine derivative or a pharmaceutically acceptable salt thereof; a preparation method thereof; and an Nrf2 activator and a pharmaceutical composition for preventing or treating diseases induced by a decrease in Nrf2 activity, both of which comprise the same as an active ingredient.

Disclosed are novel conjugates and processes for the preparation thereof. A process for the preparation of alkene-or alkyne-phosohonothiolates and -phosphonates comprises the step of: reacting a compound of formula (I) with a thiol-containing molecule of formula (II) wherein represents an amino acid, a peptide, a protein, an antibody, a nucleotide, an oligonucleotide, a saccharide, a polysaccharide, a polymer, an optionally substituted C.sub.1-C.sub.8-alkyl, an optionally substituted phenyl, or an optionally substituted aromatic 5- or 6-membered heterocyclic system; resulting in a compound of formula (III).