Ester is a chemical compound derived from an oxoacid (organic or inorganic) in which at least one –OH hydroxyl group is replaced by an –O– alkyl (alkoxy) group, 87-13-8, formula is C10H16O5, Name is Diethyl 2-(ethoxymethylene)malonate. as in the substitution reaction of a carboxylic acid and an alcohol. Quality Control of 87-13-8.
Yuan, Jing-Mei;Chen, Nan-Ying;Liao, Hao-Ran;Zhang, Guo-Hai;Li, Xiao-Juan;Gu, Zi-Yu;Pan, Cheng-Xue;Mo, Dong-Liang;Su, Gui-Fa research published 《 3-(Benzo[d]thiazol-2-yl)-4-aminoquinoline derivatives as novel scaffold topoisomerase I inhibitor via DNA intercalation: design, synthesis, and antitumor activities》, the research content is summarized as follows. Twenty-seven 3-(benzo[d]thiazol-2-yl)-4-aminoquinoline derivatives have been designed and synthesized as topoisomerase I inhibitors. The in vitro anti-proliferation evaluation against four human cancer cell lines (MGC-803, HepG-2, T24, and NCI-H460) and one normal cell line (HL-7702) indicated that most of them exhibited potent cytotoxicity. Among them, 5a(I) was identified as the most promising candidate with a low IC50 value of about 2.20 ± 0.14 and was selected for further exploration. Spectroscopic analyses and agarose-gel electrophoresis assays indicated that 5a could interact with DNA and strongly inhibit topoisomerase I (Topo I). Further screening of the Topo I activity of compounds 5b, 5c, 5e, 5f, 5h, 5i, 5j, 5l, and 5n suggested that some of the compounds might exert quite a different cytotoxicity profile to that of 5a. Mol. modeling studies confirmed that 5a adopts a unique mode to interact with DNA and Topo I. Other mol. mechanistic studies suggested that the treatment of MGC-803 cells with 5a induces S phase arrest, up-regulates the pro-apoptotic protein, down-regulates the anti-apoptotic protein, activates caspase-3, and subsequently induces mitochondrial dysfunction so as to induce cell apoptosis. The in vivo efficiency of 5a was also evaluated on MGC-803 xenograft nude mice and the relative tumor growth inhibition was 42.4% at 12 mg kg-1 without an obvious loss in the body weight
87-13-8, Diethyl ethoxymethylenemalonate is a useful research compound. Its molecular formula is C10H16O5 and its molecular weight is 216.23 g/mol. The purity is usually 95%.
Diethyl ethoxymethylidenemalonate is a matrix effect reagent used in analytical chemistry. It is often used as a substrate for the cycloaddition process, which produces malondialdehyde and hydrochloric acid. The UV-absorption of the malondialdehyde can be measured to determine the concentration of the sample. Diethyl ethoxymethylidenemalonate is also used as a dna template in binding constants, where it binds with amines to form complexes that are then analyzed by light emission. It has been shown to have an inhibitory effect on gyrase and trifluoroacetic acid, both enzymes involved in DNA replication., Quality Control of 87-13-8
Referemce:
Ester – Wikipedia,
Ester – an overview | ScienceDirect Topics