Tricyclic coumarin sulphonate derivatives with alkaline phosphatase inhibitory effects: in vitro and docking studies was written by Iqbal, Jamshed;El-Gamal, Mohammed I.;Ejaz, Syeda Abida;Lecka, Joanna;Sevigny, Jean;Oh, Chang-Hyun. And the article was included in Journal of Enzyme Inhibition and Medicinal Chemistry in 2018.Application In Synthesis of 4-Chlororesorcinol The following contents are mentioned in the article:
Tissue-nonspecific alk. phosphatase (TNAP) is an important isoenzyme of alk. phosphatases, which plays different pivotal roles within the human body. Most importantly, it is responsible for maintaining the balanced ratio of phosphate and inorganic pyrophosphate, thus regulates the extracellular matrix calcification during bone formation and growth. The elevated level of TNAP has been linked to vascular calcification and end-stage renal diseases. Consequently, there is a need to search for highly potent and selective inhibitors of alk. phosphatases (APs) for treatment of disorders associated with the over-expression of APs. Herein, a series of tricyclic coumarin sulfonate with known antiproliferative activity, was evaluated for AP inhibition against human tissue nonspecific alk. phosphatase (h-TNAP) and human intestinal alk. phosphatase (h-IAP). The methylbenzenesulfonate derivative (IC50 = 0.38 ± 0.01 μM) was found to be the most active h-TNAP inhibitor. Another 4-fluorobenzenesulfonate derivative (IC50 = 0.45 ± 0.02 μM) was found as the strongest inhibitor of h-IAP. Some of the derivatives were also identified as highly selective inhibitors of APs. Detailed structure-activity relationship (SAR) was investigated to identify the functional groups responsible for the effective inhibition of AP isoenzymes. The study was also supported by the docking studies to rationalise the most possible binding site interactions of the identified inhibitors with the targeted enzymes. This study involved multiple reactions and reactants, such as 4-Chlororesorcinol (cas: 95-88-5Application In Synthesis of 4-Chlororesorcinol).
4-Chlororesorcinol (cas: 95-88-5) belongs to organic chlorides. Organic chlorides are compounds containing a carbon-chlorine bond, which are widely used in the oil field as a wax dissolver. Aryl chlorides may be prepared by the Friedel-Crafts halogenation, using chlorine and a Lewis acid catalyst.Application In Synthesis of 4-Chlororesorcinol
Referemce:
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics