Abstract: Disclosed herein are compounds and methods for inhibiting Aha1 for the treatment of tauopathies and neurodegenerative diseases. The Aha1 inhibitor may reduce the interaction between Aha1 and Hsp90. The Aha1 inhibitor may reduce aggregation of tau protein. The Aha1 inhibitor may include a compound selected from KU-177, KU-174, and KU-308.

Abstract: An enzyme-responsive peptide and a method off using such enzyme-responsive peptide are disclosed. An enzyme-responsive peptide, the peptide comprising an amino acid having an ?-amino group, an ?-carboxylic acid group and a ?-amine group, wherein the ?-amine group is covalently bonded with a first group and the ?-carboxylic acid is covalently bonded with a second group.

Abstract: The present disclosure provides a method for preparing diselenide compound. A polar solvent is added to a dihydroflavonol compound, heated to 80° C.˜100° C., kept for 40˜50 minutes, then the base in the amount of 0.4˜1.0 times the amount of the dihydroflavonol compound is added and reacted at 80° C.˜100° C. for 5˜60 minutes, then selenium dioxide in the amount of 0.6˜1.2 times the amount of dihydroflavonol compounds at 80° C.˜100° C. The diselenide compound of the dihydroflavonol compound is obtained by reacting at a temperature of 80° C.˜100° C. for 30˜150 minutes. The method of the present disclosure has mild reaction, low pollution, does not require an anhydrous and oxygen-free environment, and is suitable for large-scale industrial production.

Abstract: A novel coumarin derivative or a pharmaceutically acceptable salt thereof and also to provide a pharmaceutical agent containing such a compound as an active ingredient is provided. The coumarin derivative or a pharmaceutically acceptable salt thereof exhibits an excellent suppressive action to the destruction of cartilage and suppressive action to the proliferation of synovial cells in a pharmacological test where the release of sulfated glycosaminoglycans (sGAG) and the proliferation of synovial cells are used as indicators whereby it is very useful as an active ingredient of a pharmaceutical composition such as a preventive or therapeutic agent for arthropathy such as osteoarthritis or chronic rheumatoid arthritis.

Abstract: Compounds represented by Formula I are provided that include synthetic transtaganolide and basiliolide products. Derivatives of these compounds and methods of synthesis are also provided.

Abstract: A compound comprising the structure: (SIG)-(SI-MOD)m. is provided in which SIG is a signaling molecule, SI is a self-immolative structure bound to SIG such that SIG has a reduced signal relative to the signal of SIG without SI, MOD is a moiety bound to SI that is subject to modification by an activator, and m is an integer from 1 to about 10. When MOD is modified by an activator, SI is destabilized and self-cleaved from SIG such that SIG generates an increased signal. Also provided are methods of determining whether a sample comprises an activator such as a nitroreductase, and methods of determining whether a mammalian cell is hypoxic using a compound of the formula (SIG)-(SI-MOD)m.

Abstract: Derivatized coumarin-based pharmaceutical compositions and methods to use them are provided. The compositions are characterized in that they inhibit the activity of tumor-related CAIX and CAXII to a greater degree than they inhibit the activity of CAI and CAII. The compositions can be used to suppress tumor growth and/or suppress tumor metastases in a mammal.

Abstract: The present invention relates to compounds of the following formula wherein R3 is a fluorescent tag. Another aspect of the invention provides an assay for determining the inhibitory effect of a test compound on an HDAC protein comprising: incubating the HDAC protein with a substrate of the above formula in the presence of a test compound; and determining the activity of the HDAC protein.

Abstract: The present invention provides methods and fluorescent compounds that facilitate detecting and labeling of a fusion protein by being capable of selectively binding to an affinity tag. The fluorescent compounds have the general formula A(B)n, wherein A is a fluorophore, B is a binding domain that is a charged chemical moiety, a protein or fragment thereof and n is an integer from 1-6 with the proviso that the protein or fragment thereof not be an antibody or generated from an antibody. The present invention provides specific fluorescent compounds and methods used to detect and label fusion proteins that contain a poly-histidine affinity tag. These compounds have the general formula A(L)m(B)n wherein A is a fluorophore, L is a linker, B is an acetic acid binding domain, m is an integer from 1 to 4 and n is an integer from 1 to 6.

Abstract: The present disclosure is directed to a reactive ester agent capable of conjugating a reporter molecule to a carrier molecule or solid support. The reactive ester agent has the general formula: wherein the variables are described throughout the application.

Abstract: The present invention relates to a process for producing 2-halogenomethylphenyl acetic acid derivatives.

Abstract: The present invention relates to compounds of the general structure: wherein Y is O, X is O, bond ? is absent and bond ? is present, or Y is H, X is CH, bond ? is present, and bond ? is absent; atom Z is a carbon and bonds ?, ? and ? are present, or is a nitrogen and bonds ?, ? and ? are absent; R1 is —H, —OH, —O—R7, —N(H)—R8, —N(H)—(CH2)n—NH2, —N(R9)(R10), or a piperazine cation; R2 is either covalently bound to R9, or is —H, or is covalently bound to R3 so as to form a substituted or unsubstituted pyrrole or R2 is covalently bound to R9 or R8 or R7; or R1 and R2 are covalently joined to form an aromatic ring; R3 is either covalently bound to R2 so as to form a pyrrole, or is, inter alia, —H, —OH, alkyl, or when Z is nitrogen R3 is ?O; R4 is, inter alia, —H, —OH, or —R11NH2; R5 is, inter alia, —H, —OH, or —R12NH2, and R6 is either is covalently bound to R10 or is —H, or R6 is covalently bound to R10 or R8 or R7.

Abstract: The present invention provides methods and fluorescent compounds that facilitate detecting and labeling of a fusion protein by being capable of selectively binding to an affinity tag. The fluorescent compounds have the general formula A(B)n, wherein A is a fluorophore, B is a binding domain that is a charged chemical moiety, a protein or fragment thereof and n is an integer from 1-6 with the proviso that the protein or fragment thereof not be an antibody or generated from an antibody. The present invention provides specific fluorescent compounds and methods used to detect and label fusion proteins that contain a poly-histidine affinity tag. These compounds have the general formula A(L)m(B)n wherein A is a fluorophore, L is a linker, B is an acetic acid binding domain, m is an integer from 1 to 4 and n is an integer from 1 to 6.

Abstract: The disclosure provides novobiocin analogues with noviose replacements which are useful as Hsp90 inhibitors in the treatment of cancer.

Abstract: HDAC inhibitors of the general formula (I) and (II) and pharmaceutically acceptable salts thereof, as described herein, are useful as inhibitors of histone deacetylases or other deacetylases, and thus are useful for the treatment of various diseases and disorders associated with acetylase/deacetylase activity as described herein (e.g., cancer). In certain embodiments, the compounds of the invention selectively target either a class or isoform of the HDAC family. Another aspect of the invention provides an assay for determining the inhibitory effect of a test compound on an HDAC protein comprising: incubating the HDAC protein with a substrate of general formula (IIIc) in the presence of a test compound; and determining the activity of the HDAC protein.

Abstract: Novel energy transfer dyes which can be used with shorter wavelength light sources are provided. These dyes include a donor dye with an absorption maxima at a wavelength between about 250 to 450 nm and an acceptor dye which is capable of absorbing energy emitted from the donor dye. One of the energy transfer dyes has a donor dye which is a member of a class of dyes having a coumarin or pyrene ring structure and an acceptor dye which is capable of absorbing energy emitted from the donor dye, wherein the donor dye has an absorption maxima between about 250 and 450 nm and the acceptor dye has an emission maxima at a wavelength greater than about 500 nm.

Abstract: Provided are a fluorescent on/off switchable compound for a gene analysis, which is highly stable and highly sensitive, and enables amplification and observation of a trace gene signal, and a labeling reagent for detection of a bio-related material, which uses the fluorescent on/off switchable compound. A compound represented by the following formula (I?): wherein X is a hydrogen atom or a carboxylic acid-protecting group, Y is a 2,4-dinitrobenzenesulfonyl group, a 2-cyano-4-nitrobenzenesulfonyl group or a 5-nitropyridin-2-ylsulfonyl group, R1, R2, R3 and R4 are each independently a hydrogen atom, a halogen atom, a hydroxyl group, an alkyl group having a carbon number of 1 to 6, an alkoxy group having a carbon number of 1 to 6, an aryl group having a carbon number of 6 to 10, or a cyano group.

Abstract: Provided is a compound that comprises the structure: where SIG is a signaling molecule and R3 is a formyl, a succinyl, a methyl succinyl, or a myristoyl. Also provided is a kit is provided that comprises the above compound, with instructions for determining the presence of the enzyme. Additionally, a method is provided for determining whether a sample has an enzyme that removes a succinyl, a methyl succinyl, a formyl, or a myristoyl moiety from an ?-amino of a lysine. Also provided is a method of determining whether a molecule inhibits an enzyme that removes a succinyl, a methyl succinyl, a formyl, or a myristoyl moiety from an ?-amino of a lysine.

Abstract: The present inventions are directed to a novel bactobolin analog bactobolin D. The present inventions also are directed to a method of producing a composition comprising at least one bactobolin analog using a bacteria strain comprising a bacterial cell comprising the biosynthetic locus of the bactobolin analog in Burkholderia thailandensis (bta cluster) or a homolog structure (at least 95% sequence identity) thereof, and further isolation and purification of the bactobolin analog. For example, the bacterial strain can be a wild type bacterial strain such as a Burkholderia strain comprising a bta cluster (e.g. Burkholderia thailandensis (e.g. E264, Bt4, and TXDOH) and Burkholderia pseudomallei (e.g. K96243, 1106a, and 1106b).

Abstract: The present invention relates to methods and reagents for detecting analytes, e.g. nucleic acids. The new methods and reagents allow a simple and sensitive detection even in complex biological samples.

Abstract: This invention provides a method for preparing a 1,2,3-triazole compound comprising contacting an organic azide with a 2-substituted-1-haloalkyne, in the presence of a copper catalyst and a copper-coordinating ligand (preferably a tertiary amine) in a liquid reaction medium, thereby forming a 1,4,5-substituted-1,2,3-triazole compound including a halo substituent at the 5-position of the triazole, the organic portion of the organic azide at the 1-position of the triazole, and the substituent of the 1-iodoalkyne at the 4-position of the triazole. A method for preparing 1-iodoalkynes is also provided.

Abstract: Provided is a compound comprising the structure: (SIG)-(SI-MOD)m. In this compound, SIG is a signaling molecule, SI is a self-immolative structure bound to SIG such that SIG has a reduced signal relative to the signal of SIG without SI, MOD is a moiety bound to SI that is subject to modification by an activator, and m is an integer from 1 to about 10. With this compound, when MOD is modified by an activator, SI is destabilized and self-cleaved from SIG such that SIG generates an increased signal. Also provided is a method of determining whether a sample comprises an activator, using the above-described compound. Additionally provided is a method of determining whether a cell comprises a nitroreductase using the above-described compound where nitroreductase is the activator. Further provided is a method of determining whether a mammalian cell is hypoxic using the above-described compound where nitroreductase is the activator.

Abstract: The present disclosure relates generally to compositions and methods for treating cancer. In some aspects, novel spirohexenolides and methods of using and producing them are described.

Abstract: The present invention relates to a process for producing 2-halogenomethylphenyl acetic acid derivatives.

Abstract: Novel compounds are provided, which are useful as linking groups in chemical synthesis, preferably in the solid phase synthesis of oligonucleotides and polypeptides. These compounds are generally photolabile and comprise protecting groups which can be removed by photolysis to unmask a reactive group. The protecting group has the general formula Y, wherein Y is a chemical structure as shown in FIG. 1. Also provided is a method of forming, from component molecules, a plurality of compounds on a support, each compound occupying a separate predefined region of the support, using the protected compounds described above.

Abstract: Disclosed herein are dithio compounds that include at least one fluorophore. The compounds additionally may include a different fluorophore or a non-fluorophore. The dithio compounds may be used as reagents for detecting thiol-containing compounds.

Abstract: Compounds of Formula 5 and prodrug compounds of Formula 5 wherein G1 is H or OH; G2 is H, R?, or CO2R?; G3, G4 and G5, are each independently selected from the group consisting of: H, R?, OH, OR?, F, Cl, Br, I, NH2, NHR?,NR?2, CN, SH, SR?, SO3H, SO3R?, SO2R?, OSO3R?, and NO2; and R? is a one to four carbon alkyl group are provided. Uses of these compounds and methods of medical treatment involving these compounds for the treatment of hepatitis C are also provided.

Abstract: The present invention is directed to compounds, pharmaceutical compositions, and methods for modulating processes mediated by AR and PR. More particularly, the invention relates to nonsteroidal compounds and compositions that are high affinity, high specificity agonists, partial agonists (i.e., partial activators and/or tissue-specific activators) and antagonists for AR and PR. Also provided are methods of making such compounds and pharmaceutical compositions, as well as critical intermediates used in their synthesis.

Abstract: The present invention relates to fluorescent dyes in general. The present invention provides a wide range of fluorescent dyes and kits containing the same, which are applicable for labeling a variety of biomolecules, cells and microorganisms. The present invention also provides various methods of using the fluorescent dyes for research and development, forensic identification, environmental studies, diagnosis, prognosis, and/or treatment of disease conditions.

Abstract: A method is presented for the preparation and use of fluorogenic peptide substrates that allows for the configuration of general substrate libraries to rapidly identify the primary and extended specificity of enzymes, such as proteases. The substrates contain a fluorogenic-leaving group, such as 7-amino-4-carbamoylmethyl-coumarin (ACC). Substrates incorporating the ACC leaving group show comparable kinetic profiles as those with the traditionally used 7-amino-4-methyl-coumarin (AMC) leaving group. The bifunctional nature of ACC allows for the efficient production of single substrates and substrate libraries using solid-phase synthesis techniques.

Abstract: A photosensitive compound has two or more structural units, in a molecule, represented by the following general formula (1): wherein R1 to R5 are selected from the group consisting of hydrogen atom, halogen atom, alkyl group, alkoxy group, acetoxy group, phenyl group, naphthyl group, and alkyl group in which a part or all of hydrogen atoms are substituted with fluorine atom; and X is a substituted or unsubstituted phenylene group or a substituted or unsubstituted naphthylene group.

Abstract: Novobiocin analogues useful as Hsp90 inhibitors in the treatment of cancer, neuroprotection, and autoimmune disorders.

Abstract: The present invention relates to an alkaline earth metal salt or an organic amine salt of a compound represented by the formula [I]: wherein R1 and R2 are each a hydrogen atom, a halogen atom, or an optionally substituted linear hydrocarbon group; ring A is an optionally further substituted benzene ring; B is an optionally substituted benzene ring; R is a carboxyl group or a linear hydrocarbon group substituted with a carboxyl group and the like.

Abstract: A compound represented by the general formula (I) below: In the formula, A is as defined in the specification and B denotes where n is an integer of 1 to 4, and a process for producing the above compound includes a reaction between an activated ester and a t-butoxycarbonylaminoethylamine or an ?-amino acid derivative.

Abstract: The present invention is directed to substituted coumarins and quinolines and analogs thereof, represented by the general Formula I: wherein A, B, X, Y, and Z are defined herein. The present invention also relates to the discovery that compounds having Formula I are activators of caspases and inducers of apoptosis. Therefore, the activators of caspases and inducers of apoptosis of this invention can be used to induce cell death in a variety of clinical conditions in which uncontrolled growth and spread of abnormal cells occurs.

Abstract: The invention is directed to a new class of quinolin-zene and z-exc chromen compounds that have been derivatized at the 6-position with a urea or this urea moet, and to then use as androgen antagonists.

Abstract: An inhibitor for 20-hydroxyeicosatetraenoic acid production which comprises as the active ingredient a specific hydroxyformamidine derivative or a pharmacologically acceptable salt thereof. It is useful especially as a remedy for kidney diseases, cerebrovascular diseases, or circulatory diseases. The novel hydroxyformamidine derivative or pharmacologically acceptable salt thereof is also provided.

Abstract: A fluorescent compound, suitable for use in an active layer of an organic light-emitting device and exhibiting both good luminescence and excellent thermal stability, which has the structure wherein R is substituted or unsubstituted alkyl; wherein Ar2 is optionally present; and wherein Ar1, Ar2, and Ar3 are independently each a substituted or unsubstituted aryl group.

Abstract: The present invention provides a novel dioxin analogue for use in the search for organisms capable of degrading dioxin.

Abstract: Compounds which are non-natural galanin receptor ligands are disclosed. The ligands are of small size, have agonist or antagonist galanin activity and may cross the blood-brain barrier to displace galanin from galanin receptors. The ligands are useful as medicaments for treatment of convulsions (e.g. in epilepsy), diseases and disorders related to endocrinology (e.g., growth hormone, insulin or prolactin release), tumors expressing galanin receptors, feeding disorders pain, allodynia, psychiatric disorders such as depression (involving e.g., noradrenaline or serotonin), cognitive disorders (e.g. Alzeimer's disease), and the like.

Abstract: A method is presented for the preparation and use of fluorogenic peptide substrates that allows for the configuration of general substrate libraries to rapidly identify the primary and extended specificity of enzymes, such as proteases. The substrates contain a fluorogenic-leaving group, such as 7-amino-4-carbamoylmethyl-coumarin (ACC). Substrates incorporating the ACC leaving group show comparable kinetic profiles as those with the traditionally used 7-amino-4-methyl-coumarin (AMC) leaving group. The bifunctional nature of ACC allows for the efficient production of single substrates and substrate libraries using solid-phase synthesis techniques. The approximately 3-fold increased quantum yield of ACC over AMC permits reduction in enzyme and substrate concentrations. As a consequence, a greater number of substrates can be tolerated in a single assay, thus enabling an increase in the diversity space of the library.

Abstract: Methods are provided for treatment of eye disorders and injury, including methods for treatment of reduced flow of blood or other nutrients to retinal tissue and/or optic nerve, methods for treatment of retinal ischemia and trauma and methods for treatment for optic nerve injury/damage.

Abstract: A series of activated iodo-benzamide derivatives are described as antineoplastic and antiviral drug compounds. The compounds generally possess a chelating group, a thiol trapping group and an activating group. The presumptive mechanism of action in preventing cancer cell and virus replication is through inhibition of the binding of transcription factors to zinc finger binding domains. The compounds are effective in inhibiting growth of a variety of human and animal tumor and leukemia cell lines at low concentrations.

Abstract: An organic light emitting display is provided which comprises as an emitting layer a fluorescent dye having at least one amine moiety substituted with two aryl groups. Also provided are new fluorescent compounds having N-aryl substituents which exhibit reduced pH sensitivity and enhanced stability to protonation.

Abstract: This invention concerns an enzyme substrate consisting of a target part and a marker part, hydrolysis of the substrate leading to separation of the target part from the marker part, and said target part being specific for the enzyme activity being assayed. It also concerns a formulation containing at least one such substrate, and a method for detecting the bacterial species Pseudomonas aeruginosa.

Abstract: The present invention relates to a novel flavone derivative, pharmaceutically acceptable salt, hydrate, solvate and isomer thereof which is useful as an inhibitor against Cyclin Dependent Kinase (CDK), a process for preparation thereof, and a composition of anti-cancer agent or agent for treating neurodegenerative disease comprising this compound as an active ingredient.

Abstract: A target gene can be expressed site-specifically and with desired timing without damaging the cell itself or inducing mutation in a nucleic acid molecule within the cell. Expression of the above target gene is suppressed by allowing a caging agent represented by the following formula (1) to bind to a nucleic acid molecule containing the target gene; and the suppression of expression of the above target gene is cancelled by detaching the caging agent from the above nucleic acid molecule by UV-illumination.

Abstract: Disclosed are pyran derivatives, which have distinctive sensitivity to visible light and distinctive luminous ability. The derivatives are useful in photopolymerization, electroluminescence, and dye lasers, and are obtainable through a step of reacting a compound having a 4-cyanomethylene-2-methyl-4H-pyran skeleton with a compound having a 3-formylcoumarin skeleton.

Abstract: An organic light emitting display is provided which comprises as an emitting layer a fluorescent dye having at least one amine moiety substituted with two aryl groups. Also provided are new fluorescent compounds having N-aryl substituents which exhibit reduced pH sensitivity and enhanced stability to protonation.

Abstract: Methods are provided for treatment of eye disorders and injury, including methods for treatment of reduced flow of blood or other nutrients to retinal tissue and/or optic nerve, methods for treatment of retinal ischemia and trauma and methods for treatment for optic nerve injury/damage.