Building Blocks

2,4-Dimethoxyiodobenzene is a methyl ketone that has three methoxy groups. It is used as a building block in organic synthesis and can be synthesized by the reaction of 2,4-dimethoxybenzaldehyde with peroxide and methylamine. 2,4-Dimethoxyiodobenzene inhibits radical formation by reacting with an activated metal halide to form a covalent bond between the two molecules. The terminal alkyne reacts with a halogen to form an alkynyl radical which then reacts with another activated metal halide to form a second covalent bond. This process creates a new radical that has been deactivated by the addition of two bonds, preventing it from initiating another chain reaction. 2,4-Dimethoxyiodobenzene also exhibits inhibitory potency against β-amino acid decomposition through the same mechanism.

1,1-Dioxido-1-benzothien-6-ylamine is a cytotoxic drug that inhibits the synthesis of DNA and RNA in cancer cells. It is synthesized from benzo[c]thiophene-2,5-dione by oxidation with nitric acid to give the corresponding dioxido compound. The synthesized product has high lipophilicity (log P = 2.2) and a reactive hydroxy group that can undergo modifications such as esterification or alkylation. 1,1-Dioxido-1-benzothien-6-ylamine shows potent antitumor activity against solid tumours and high lipophilicity that enables it to cross the blood brain barrier very easily. It also induces apoptosis in tumour cells by binding to nucleic acids and inhibiting their synthesis. This drug is cytotoxic at nanomolar concentrations and has been shown to be effective against lung

5-Methoxy-benzo[b]thiophene is a synthetic compound that has been shown to have antiestrogenic activity. It was synthesized using the acetonitrile technique and has been shown to inhibit the growth of mammary carcinomas in mice. 5-Methoxy-benzo[b]thiophene binds to estrogen receptor protein, which inhibits the binding of estrogen and prevents its effects on breast cancers. This agent also has been shown to be an effective therapy for some human breast cancer cells, which may be due to its ability to block estrogen receptor function.