Building Blocks

Versatile small molecule scaffold

Versatile small molecule scaffold

Versatile small molecule scaffold

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Versatile small molecule scaffold

Versatile small molecule scaffold

2-Bromo-3,3,3-trifluoro-1-propene is a chemical compound that has been synthesized in an asymmetric reaction. The reactant is bromopropane and the product is 2,2,2-trifluoropropene. The methylene group on the propene molecule is activated by the nucleophilic attack of a fluoride ion from hydrogen fluoride to form a cavity with a highly strained bond. The kinetic study of this reaction revealed that the activation energy for the reaction is 42 kJ/mol. Palladium-catalyzed coupling reactions are catalyzed by palladium and require nonpolar solvents such as toluene or dichloromethane. This type of reaction has been shown to be exothermic with an isolated yield of 1%.

Boc-His(Trt)-OH is a chemical compound that has been used in the laboratory to study uptake and binding of compounds. It is stable in complex with albumin, which has led to its use as a model system for studying hepatic steatosis. This chemical can be synthesized by solid-phase synthesis with trifluoroacetic acid and polypeptide synthesis. FT-IR spectroscopy has been used to characterize Boc-His(Trt)-OH, revealing its chemical diversity.

1,2-Bis(chlorodimethylsilyl)ethane is a reactive chemical that is synthesized from hydroxychloroformates and hydrogen chloride. It reacts with silicon to form chlorosilanes, which are then used in the polymerization of siloxanes. 1,2-Bis(chlorodimethylsilyl)ethane has been shown to be an effective initiator for the polymerization of methyl methacrylate and ethylene glycol dimethacrylate. 1,2-Bis(chlorodimethylsilyl)ethane is also used as a hydroxyl group donor in organic reactions.

Versatile small molecule scaffold

Versatile small molecule scaffold

Cabozantinib is a small molecule that is the first to target VEGFR-2, which is a receptor tyrosine kinase involved in the development of fibrosis. Cabozantinib inhibits the activity of VEGFR-2 by binding to its ATP-binding site and blocking the phosphorylation of downstream signaling pathways. Cabozantinib has been shown to have antifibrotic properties in both preclinical and clinical models. The drug candidate has been shown to reduce kidney fibrosis in animal models. The standard dose for cabozantinib was found to be 5 mg/kg, with a maximum tolerated dose of 20 mg/kg. In vitro studies have indicated that cabozantinib binds with high affinity to the ATP-binding pocket of VEGFR-2, exhibiting competitive inhibition against other kinases such as PDGFR-beta and cKit, as well as diaryliodonium (a specific inhibitor). Caboz

Versatile small molecule scaffold

Versatile small molecule scaffold

Versatile small molecule scaffold

Versatile small molecule scaffold

Versatile small molecule scaffold

4-Chloro-8-quinolinol is a quinoline derivative that has been shown to have pharmacological effects. It is used in the synthesis of other compounds, such as 5-chloro-8-hydroxyquinoline, which is used in the treatment of cancer. 4-Chloro-8-quinolinol can also be prepared by oxidizing 5,6,7,8 tetrachloroquinoline with chlorine and ammonia. The photophysical properties of this compound are analogous to those of benzothiazole derivatives. The fluorescence emission spectrum ranges from 360 nm to 450 nm with a maximum at 390 nm and emission intensity at 350 nm. This compound exhibits fungitoxicity against Penicillium notatum and Aspergillus fumigatus.

1,1'-Carbonimidoylbis-1H-imidazole is a ligand that binds to amines and isosteres. It can be activated with electrophilic reagents to form an activated linker. This ligand has been shown to inhibit the growth of xenograft tumor cells in mice by binding to functional groups on the cell surface. This drug also has been shown to bind to the receptor for advanced glycation end products (RAGE) and inhibit its function. 1,1'-Carbonimidoylbis-1H-imidazole has also been evaluated as a cancer therapeutic agent in animal models.