85302-08-5

Upstream product

• 493-72-1 5-phenyl-cyclohexane-1,3-dione 
• 4637-24-5 N,N-dimethyl-formamide dimethyl acetal 
• 122-57-6 1-Phenylbut-1-en-3-one 
• 100-51-6 benzyl alcohol 
• 100-52-7 benzaldehyde 

Downstream Products

• 87379-59-7 3-Hydroxy-2-iminomethyl-5-phenyl-cyclohex-2-enone 
• 64500-73-8 2,5-dioxo-7-phenyl-1,2,5,6,7,8-hexahydro-quinoline-3-carbonitrile 
• 84548-16-3 5,6,7,8-Tetrahydro-7-phenyl-2,5-dioxo-2H-1-benzopyran-3-carboxamide 
• 87379-53-1 2-Methyl-7-phenyl-7,8-dihydro-6H-quinazolin-5-one 
• 29974-41-2 2.7-Diphenyl-5-oxo-5.6.7.8-tetrahydrochinazolin 
• 50839-31-1 1,6-diphenyl-1,5,6,7-tetrahydro-indazol-4-one 
• 85302-18-7 1-Methyl-6-phenyl-1,5,6,7-tetrahydro-indazol-4-one 
• 1296687-86-9 1-(4-fluoro-phenylamino)-2,5-dioxo-7-phenyl-1,2,5,6,7,8-hexahydro-quinoline-3-carbonitrile 
• 1296687-84-7 2,5-dioxo-7-phenyl-1-phenylamino-1,2,5,6,7,8-hexahydroquinoline-3-carbonitrile 

Relevant academic research and scientific papers

Inhibition studies on carbonic anhydrase isoforms I, II, IV and IX with N-arylsubstituted secondary sulfonamides featuring a bicyclic tetrahydroindazole scaffold

Carbonic Anhydrases (CAs) are pharmaceutically relevant targets for the treatment of several disease conditions. The ubiquitous localization of these enzymes and the high homology shared by the different isoforms represent substantial impediments for the

Tetrahydroquinazole-based secondary sulphonamides as carbonic anhydrase inhibitors: synthesis, biological evaluation against isoforms I, II, IV, and IX, and computational studies

A library of variously decorated N-phenyl secondary sulphonamides featuring the bicyclic tetrahydroquinazole scaffold was synthesised and biologically evaluated for their inhibitory activity against human carbonic anhydrase (hCA) I, II, IV, and IX. Of not

Inhibition of Autophagy by a Small Molecule through Covalent Modification of the LC3 Protein

The autophagic ubiquitin-like protein LC3 functions through interactions with LC3-interaction regions (LIRs) of other autophagy proteins, including autophagy receptors, which stands out as a promising protein–protein interaction (PPI) target for the intervention of autophagy. Post-translational modifications like acetylation of Lys49 on the LIR-interacting surface could disrupt the interaction, offering an opportunity to design covalent small molecules interfering with the interface. Through screening covalent compounds, we discovered a small molecule modulator of LC3A/B that covalently modifies LC3A/B protein at Lys49. Activity-based protein profiling (ABPP) based evaluations reveal that a derivative molecule DC-LC3in-D5 exhibits a potent covalent reactivity and selectivity to LC3A/B in HeLa cells. DC-LC3in-D5 compromises LC3B lipidation in vitro and in HeLa cells, leading to deficiency in the formation of autophagic structures and autophagic substrate degradation. DC-LC3in-D5 could serve as a powerful tool for autophagy research as well as for therapeutic interventions.

A CLASS OF ISOINDOLONE-IMIDE RING-1,3-DIONE-2-ENE COMPOUNDS, COMPOSITION AND USE THEREOF

The present invention provides an isoindolone-imide ring-1,3-dione-2-ene compound, and a preparation method, a pharmaceutical composition and use thereof. Specifically, the present invention provides a compound of Formula (I) below or a pharmaceutically a

USE OF AMINOMETHYLENECYCLOHEXANE-1,3-DIONE COMPOUND

The present invention relates to use of an aminomethylenecyclohexane-1,3-dione compound, more particularly to use of a compound shown in the following formula (I) or a pharmaceutically acceptable salt thereof alone or in combination with other drug in pre

COMPOUND USED AS AUTOPHAGY REGULATOR, AND PREPARATION METHOD THEREFOR AND USES THEREOF

It is related to compounds used as autophagy modulators and a method for preparing and using the same, specifically providing a compound of general formula (I), or pharmaceutically acceptable salts thereof, which is a type of autophagy modulators, particularly mammalian ATG8 homologues modulators.

Tetrahydroquinazoline derivatives and pharmaceutical composition for preventing or treating psoriasis comprising the same

The present invention relates to a tetrahydroquinazoline derivative and a pharmaceutical composition for preventing or treating psoriasis containing the same as an active ingredient. The compound provided in one aspect of the present invention has an effe

4-Substituted Benzenesulfonamides Incorporating Bi/Tricyclic Moieties Act as Potent and Isoform-Selective Carbonic Anhydrase II/IX Inhibitors

As a part of our efforts to expand chemical diversity in the carbonic anhydrases inhibitors (CAIs), three small series of polyheterocyclic compounds (4-6) featuring the primary benzenesulfonamide moiety linked to bi/tricyclic scaffolds were investigated. Highly effective inhibitors against the target tumor-associated hCA IX (low nanomolar/subnanomolar potency levels) showing significant functional selectivity profile toward hCA I, II, and IV isozymes were identified. Molecular docking studies clarified the reasons behind the activity and selectivity of the new compounds.

REMOVAL OF SENESCENCE-ASSOCIATED MACROPHAGES

In various aspects and embodiments provided are compounds, compositions and methods relating to aging, senescent cells (SCs) and/or senescence associate macrophages (SAMs). In certain aspects and embodiments provided are compounds and compositions that selectively kill or reprogram senescent cells (SCs) and or senescence associate macrophages (SAMs) and associated methods. In some embodiments, the compounds compositions and methods treat or reverse aging and/or age-related diseases.

Pathways for cyclizations of hydrazine-derived 2-(2-cyanovinyl)-3-oxo- cyclohex-1-ene enolates

The introduction of a hydrazine functionality into 2-(2-cyanovinyl)-3-oxo- cyclohex-1-ene enolates results in their spontaneous cyclizations with participation of the hydrazine moiety. Depending on the reaction conditions used, the hydrazine-derived enola