Easmon, Johnny; Heinisch, Gottfried; Puerstinger, Gerhard; Langer, Thierry; Oesterreicher, Juergen K.; Grunicke, Hans H.; Hofmann, Johann published the artcile< Azinyl and Diazinyl Hydrazones Derived from Aryl N-Heteroaryl Ketones: Synthesis and Antiproliferative Activity>, Quality Control of 112-63-0, the main research area is azinyl hydrazone preparation antiproliferative activity; hydrazone diazinyl preparation antiproliferative activity; antiproliferative structure activity azinyl hydrazone preparation.
A series of N-heteroaryl hydrazones derived from aryl N-heteroaryl or bis-N-heteroaryl methanones was prepared in search for potential novel antitumor agents. The stereochem. of these compounds was established by NMR. Antiproliferative activity was determined in a panel of human tumor cell lines (CCRF-CEM, Burkitt’s lymphoma, HeLa, ZR-75-1, HT-29, and MEXF 276L) in vitro. Generally, the new compounds were more potent (IC50 = 0.011-0.436 μM) than the ribonucleotide reductase inhibitor hydroxyurea (IC50 = 140 μM). Most of the compounds exhibited the highest activity against Burkitt’s lymphoma with IC50 = 0.011-0.035 μM. [14C]Cytidine incorporation into DNA was quantitated for selected hydrazones as a measure of the inhibition of ribonucleotide reductase in Burkitt’s lymphoma cells. (E)-Hydrazones inhibit [14C]cytidine incorporation to a greater extent (IC50 = 0.67-5.05 μM) than the (Z)-isomers (IC50 = 7.20 to >10 μM). Principal component anal. of the IC50 values obtained for inhibition of cell proliferation revealed that the cell lines tested can be grouped into three main families showing different sensitivities toward the compounds in our series (i, CCRF-CEM, Burkitt’s lymphoma, and HeLa; ii, HT-29; and iii, MEXF 276 L).
Journal of Medicinal Chemistry published new progress about Cytotoxic agents. 112-63-0 belongs to class esters-buliding-blocks, and the molecular formula is C19H34O2, Quality Control of 112-63-0.
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