Building Blocks

Versatile small molecule scaffold

4-(tert-Butyl)-2-chloropyridine is a ligand that has been used in the synthesis of a number of boronic acids and quinoline derivatives. It is also useful in cross-coupling reactions, which are nucleophilic substitution reactions involving two partners, such as an organometallic reagent and an organic halide or pseudohalide. The linker can be any group that connects the two partners together for these reactions. 4-(tert-Butyl)-2-chloropyridine is stable under acidic conditions, making it an excellent choice for coupling with amines to produce amides.

5-Methyl-1H-indazol-4-amine is a tyrosine kinase inhibitor that has been shown to be potent in inhibiting the activity of various types of tyrosine kinases. It has good oral pharmacokinetics and is not metabolized by the liver. 5-Methyl-1H-indazol-4-amine binds to the ATP site on the enzyme and prevents phosphorylation, which inhibits cell proliferation and growth. This agent also inhibits DNA synthesis, protein synthesis, and phosphoinositide turnover in cells. 5-Methyl-1H-indazol-4-amine is an orally active inhibitor of tyrosine kinases with good oral pharmacokinetics and does not require metabolic activation by the liver. This agent may be used for the treatment of cancer or other diseases associated with uncontrolled cell growth.

Versatile small molecule scaffold

Versatile small molecule scaffold

Versatile small molecule scaffold

Versatile small molecule scaffold

1-Ethynyl-4-(methylsulfanyl)benzene (EMSB) is a novel organometallic compound that has been shown to be an inhibitor of cyclooxygenases. EMSB inhibits cox-1 and cox-2, which are enzymes involved in the inflammatory response. Inhibiting these enzymes may lead to the reduction of inflammation, which is implicated in many diseases such as cancer, arthritis, and cardiovascular disease. EMSB has also been shown to have antiinflammatory activity in a gravimetric analysis of human neutrophils. This molecule has been shown to inhibit the production of prostaglandins by inhibiting the enzyme cyclooxygenase and x-ray diffraction data show that this molecule binds with high affinity to cox-1 and cox-2.

Versatile small molecule scaffold

7-Benzyl-2,6-dichloro-7H-purine is a reagent that is used in the synthesis of adenine and other purines. It can be synthesized by coupling 3-methylxanthine with aminoacids and organometallic reagents. This chemical can also be used to selectively synthesize 6-benzyladenine, which is an important precursor to pharmaceuticals. The 7-benzyl group on this chemical has been shown to act as a positional group in the catalytic hydrogenation of amines. This selective hydrogenation process has been found to be regioselective for cycloalkyl amines.

Versatile small molecule scaffold

Rhosin hydrochloride is a cardiac glycoside derived from the plant Rhosinus peregrinus. It has been shown to have a regulatory effect on cardiac hypertrophy, and has been used in animal experiments to treat cancer. Rhosin hydrochloride is also known to inhibit cell factor and regulatory adhesions, which are proteins that aid in the binding of cells to other cells or tissue. It has been shown to be effective at inhibiting the uptake of calcium ions by rat cardiomyocytes. These properties make rhosin hydrochloride an attractive target for future research into cardiovascular disease treatment.

Versatile small molecule scaffold

Versatile small molecule scaffold

Versatile small molecule scaffold

Versatile small molecule scaffold

Versatile small molecule scaffold

5-fluoro-1H-pyrazolo[3,4-b]pyridine is a medicament for the treatment of cardiovascular diseases and cardiovascular disorders. It is in the form of a powder that is to be taken orally. 5-fluoro-1H-pyrazolo[3,4-b]pyridine has been shown to have an effect on inhibition of platelet aggregation and vasodilation.