Mutations in oncogenes and tumor suppressors contribute to the development and progression of cancer. The present disclosure describes compounds and methods that restore DNA binding affinity of p53 mutants. The compounds of the present disclosure can bind to mutant p53 and restore the ability of the p53 mutant to bind DNA and activate downstream effectors involved in tumor suppression. The disclosed compounds can be used to reduce the progression of cancers that contain a p53 mutation.

Mutations in oncogenes and tumor suppressors contribute to the development and progression of cancer. The present disclosure describes compounds and methods that restore DNA binding affinity of p53 mutants. The compounds of the present disclosure can bind to mutant p53 and restore the ability of the p53 mutant to bind DNA and activate downstream effectors involved in tumor suppression. The disclosed compounds can be used to reduce the progression of cancers that contain a p53 mutation.

Disclosed are a benzyl piperazine compound, a preparation method there for and an application thereof in an antivirus. The benzyl piperazine compound has a structure represented by the following general formula(I). It is proven by experiments that the benzyl piperazine compound not only has significant antiviral activity, but also has the advantages of low cytotoxicity, a high selectivity index and soon.

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Disclosed are a benzyl piperazine compound, a preparation method there for and an application thereof in an antivirus. The benzyl piperazine compound has a structure represented by the following general formula(I). It is proven by experiments that the benzyl piperazine compound not only has significant antiviral activity, but also has the advantages of low cytotoxicity, a high selectivity index and soon.

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The present invention relates to a composition for use in preventing migration of cancer cells in a subject known or suspected to suffer from cancer, the composition comprising at least one metal complex having the structure (I), formula (I), wherein M is a metal, preferably selected from the group consisting of copper, iron, manganese and zinc, X is X.sup.a or X.sup.b, wherein X.sup.a is selected from the group consisting of O, S and —N(R.sup.1)—, wherein R.sup.1 is H or alkyl, and wherein X.sup.b is a group forming a coordinate covalent bond to a second metal M′, preferably a group O, S or —N(R.sup.1)—, wherein M′ is preferably selected from the group consisting of copper, iron, manganese and zinc, and wherein M′ and M may be the same or different and are preferably the same, Z.sup.1 and Z.sup.2 are independently of each other a, substituted or unsubstituted, -Aryl-O—, -Aryl-N— or heteroaryl group, Y is Y.sup.a or Y.sup.b, wherein Y.sup.a is selected from the group consisting of H, alkyl, —OH, —SH, halogen, and —NR.sup.3R.sup.4, wherein R.sup.3 and R.sup.4, are independently of each other selected from H and alkyl, preferably R.sup.3 and R.sup.4 are both H, and wherein Y.sup.b is a group forming a coordinate covalent bond to M or M′, preferably Y.sup.b is a group O, S or —N(R.sup.Yb1R.sup.Yb2), wherein R.sup.Yb1 and R.sup.Yb1, are, independently of each other, H or alkyl, preferably H, and wherein n and m are integers, which are independently of each other, 0 or 1, Y.sup.2 is water or a halogen, and wherein Y.sup.3 is water or a halogen. The present invention further relates to a combined preparation comprising the aforesaid composition as well as to an in vitro method, for determining whether cancer cells are susceptible to immobilizing by the aforesaid compound.

##STR00001##

The present invention relates to sulfonylureas and sulfonylthioureas comprising a 5-membered nitrogen-containing heteroaryl ring attached to the sulfonyl group, wherein the heteroaryl ring is substituted with a nitrogen-containing group R.sup.1′ wherein R.sup.1 contains from 1 to 7 atoms other than hydrogen or halogen. The present invention further relates to salts, solvates and prodrugs of such compounds, to pharmaceutical compositions comprising such compounds, and to the use of such compounds in the treatment and prevention of medical disorders and diseases, most especially by the inhibition of NLRP.sub.3.

Described are compounds, compositions, and methods suitable for diagnosing individuals with eye injuries and/or diseases. The compounds of the present disclosure have fluorescent groups and bis-dipicolylamine groups, which may be substituted or unsubstituted. The fluorescent group and bis-dipicolylamine group are connected by linking groups. The compositions may be formulated and administered as an eye drop. The methods may be used to track and/or label dying cells associated with eye injuries and/or diseases, such as, for example, retinal degenerations including, but not limited to, retinitis pigmentosa, glaucoma, diabetic retinopathy, and age-related macular degeneration.

The present disclosure provides compounds, pharmaceutically acceptable compositions thereof, and methods of using the same.

Provided is an process for the automated synthesis of at least one chemical compound including providing at least one substrate in at least one solvent in the at least one reaction container; automatically passing the at least one substrate through at least one first compartment of the at least one cartridge once or several times and collecting a formed substrate-reagent intermediate product in the at least one reaction container prior to passing the substrate-reagent intermediate product into a subsequent compartment; automatically passing the substrate-reagent intermediate product through at least one second compartment once or several times and collecting a formed reaction product prior to passing the reaction product into a subsequent compartment; automatically passing the reaction product through at least one third compartment for purifying the product once or several times and collecting a purified product in the at least one reaction container.

Provided is an process for the automated synthesis of at least one chemical compound including providing at least one substrate in at least one solvent in the at least one reaction container; automatically passing the at least one substrate through at least one first compartment of the at least one cartridge once or several times and collecting a formed substrate-reagent intermediate product in the at least one reaction container prior to passing the substrate-reagent intermediate product into a subsequent compartment; automatically passing the substrate-reagent intermediate product through at least one second compartment once or several times and collecting a formed reaction product prior to passing the reaction product into a subsequent compartment; automatically passing the reaction product through at least one third compartment for purifying the product once or several times and collecting a purified product in the at least one reaction container.