Building Blocks

2-Oxo-2H-chromene-6-sulfonamide is a coumarin derivative that has been shown to have pro-apoptotic properties. It induces apoptosis, or programmed cell death, in hepg2 cells by inhibiting the synthesis of proteins that are necessary for the growth and survival of cancer cells. 2-Oxo-2H-chromene-6-sulfonamide also inhibits the function of annexin and mcf7, two proteins involved in apoptosis. This drug has been shown to be effective against breast cancer cells in vitro. In addition, 2-Oxo-2H-chromene-6-sulfonamide has been found to inhibit the growth of human ovarian cancer cells in vivo. The toxicity studies on this drug have not yet been conducted on humans; therefore, it is not approved for use as a therapeutic agent.

Versatile small molecule scaffold

Phenyl-1,2,4-oxadiazole-5-carbohydrazide (POD) is a heterocycle that has analgesic properties. It is an analgesic agent that belongs to the group of arylidene hydrazides. POD binds to the opioid receptors in the brain, which causes pain relief. POD is structurally related to dipyrone and has similar pharmacological profile. The drug was shown to be effective in reducing constrictions in guinea pigs and rats.

Versatile small molecule scaffold

Versatile small molecule scaffold

3-Methanesulfinylbenzoic acid is an active site molecule that catalyzes the demethylation of alkylamines, amides, and cyclic sulfur compounds. The enzyme has been shown to have monooxygenase activity and can be biotransformed by various reactions including n-oxide formation, hydroxylation, sulfoxidation, and deamination. 3-Methanesulfinylbenzoic acid is a bacterial enzyme that has been crystallized in the x-ray crystal structures of both oxidized and reduced forms. The enzyme functions as a homodimer with a molecular weight of approximately 67 kDa.

Versatile small molecule scaffold

Indolizine-1-carboxylic acid (IDCA) is an antimicrobial agent that inhibits bacterial growth by interfering with the synthesis of proteins. IDCA is a fluorescent compound that can be detected using fluorescence spectroscopy. This drug has been shown to have potent cytotoxic effects against cancer cells, as well as antibacterial activity against Staphylococcus aureus and other bacteria.

Versatile small molecule scaffold

Versatile small molecule scaffold

Versatile small molecule scaffold

Versatile small molecule scaffold

Versatile small molecule scaffold

7-Chloro-benzo[b]thiophene is a nicotinic acetylcholine receptor antagonist that binds to the receptor and blocks its activation. 7-Chloro-benzo[b]thiophene has been shown to be effective in treating Alzheimer's disease in humans, as well as ameliorating the symptoms of schizophrenia in animals. It has also been shown to bind to acetylcholine receptors with high affinity. This drug is an amide derivative of mercaptoacetic acid and an acetylcholine molecule. 7-Chloro-benzo[b]thiophene binds to the receptor at the site where acetylcholine would normally bind, and blocks its activation by preventing the binding of acetylcholine molecules.

2-Bromo-3-nitrobenzyl alcohol is a lysergic acid derivative that undergoes an intramolecular cyclisation to form a triamide. This reaction can be catalysed by phosphoric acid, chloroform, or mercaptoacetic acid. The hydroxyl group and nitro group are both nucleophilic, making this reaction very useful in organic synthesis. 2-Bromo-3-nitrobenzyl alcohol has been used to synthesise dihydroindoles with high yield.

Versatile small molecule scaffold

Versatile small molecule scaffold

Versatile small molecule scaffold