Building Blocks

Versatile small molecule scaffold

Versatile small molecule scaffold

Versatile small molecule scaffold

Versatile small molecule scaffold

Versatile small molecule scaffold

5-Iodo-2-methoxypyrimidine is an enantioenriched, modular, polyfunctionalized, derivatized molecule that has been shown to be both antiproliferative and selective. It is synthesized in a two step reaction from acetate and 2-iodo-5-methoxypyridine via the use of a coupling agent, such as HATU. The synthesis proceeds with an arylation followed by a decarboxylative coupling reaction. This synthetic method produces 5-iodo-2-methoxypyrimidine in high yields with excellent enantioselectivity.

2,3-Dihydro-5(1H)-indolizinone (NU-120) is a quinoid compound that has been shown to have anti-oxidant and anti-inflammatory properties. The prodrug form of NU-120 is converted to the active n-oxide form in vivo by the enzyme cytochrome P450. This conversion takes place at an efficient rate with oral absorption between 0.2% and 2%. The drug has a crystalline structure and solvates readily in water.

2-[Benzyl(methyl)ao]propanoic acid is a glycine analogue that has been synthesized and characterized. It is an α-amino acid with the chemical formula C5H11NO2. The molecule has a chiral carbon atom at the center of the propanoic acid group and contains two asymmetric carbon atoms on the benzene ring, which enable it to exist in two stereoisomers. The compound has been shown to exhibit interligand interactions with copper as well as stereoselectivity in its interactions with l-amino acids. 2-[Benzyl(methyl)ao]propanoic acid also exhibits dichroism spectra, which are unique to these types of molecules.

Versatile small molecule scaffold

Versatile small molecule scaffold

Versatile small molecule scaffold

Versatile small molecule scaffold

Versatile small molecule scaffold

Versatile small molecule scaffold

Versatile small molecule scaffold

Versatile small molecule scaffold

1-Bromo-4-N-phthalimido-2-butanone is a quinazolinone that has been shown to be active against a number of bacterial strains, including Staphylococcus aureus, Salmonella typhi, and Escherichia coli. It also has cytotoxic effects on the human breast cancer cell line MCF-7. 1-Bromo-4-N-phthalimido-2-butanone has been shown to inhibit the growth of human prostate cancer cells by binding to the DNA in these cells and inhibiting RNA synthesis. This drug also prevents the development of influenza A virus in mice by acting as an analgesic and an antitumor agent. The antiinflammatory activities of 1BBA may be due to its inhibition of prostaglandin synthesis.

Versatile small molecule scaffold

Versatile small molecule scaffold

2-Carboxyethyl(triphenyl)phosphonium bromide is a phosphonium salt that inhibits the adenosine receptors. It is also shown to have anti-cancer effects on cells. 2-Carboxyethyl(triphenyl)phosphonium bromide has been shown to inhibit the growth of cancer cells in cell culture and in animal models. It has been proposed as a potential therapeutic agent for neurodegenerative diseases, such as Parkinson's disease and Huntington's disease, due to its ability to inhibit the activity of the enzyme formylation. The drug binds to nucleophilic sites on proteins, which may be due to its structure activity relationship with adenosine receptors. The synthesis of this drug involves ethyl formate as a starting material, which undergoes an amination reaction with diisobutylaluminium followed by formylation with dibromomethane in acid catalyst conditions.