Eissa, Ibrahim H. published the artcileDesign and Discovery of Novel Quinoxaline Derivatives as Dual DNA Intercalators and Topoisomerase II Inhibitors, Quality Control of 116-63-2, the publication is Anti-Cancer Agents in Medicinal Chemistry (2018), 18(2), 195-209, database is CAplus and MEDLINE.
Backgroun/Methods: In attempt to develop new potent antitumor agents, a series of quinoxaline derivatives was designed and synthesized. The novel compounds were tested in vitro for their antiproliferative activities against HePG2, MCF7 and HCT116 cell lines. Addnl., DNA binding affinities as well as DNAtop II inhibitory activities of the synthesized compounds were investigated as potential mechanism for anticancer activity. Compounds 13, 15, 16 and 19 exhibited good cytotoxicity activities against the three cell lines (IC50 ranging from 7.6 to 32.4 muM) comparable to that of doxorubicin (IC50 = 9.8 muM). Results: Interestingly, the results of DNA binding and DNAtop II inhibition assays were in agreement with those of the cytotoxicity tests, where the most potent anticancer compounds showed good DNA binding affinities (IC50 ranging from 25.1 to 32.4 muM) and DNAtop II inhibitory activities (IC50 ranging from 6.4 to 15.3 muM) comparable to those of doxorubicin (IC50 = 28.1 and 3.8 muM, resp.). Furthermore, mol. docking studies were carried out for the new compounds in order to investigate their binding pattern with the prospective target, DNAtop II complex (PDBcode: 3qx3).
Anti-Cancer Agents in Medicinal Chemistry published new progress about 116-63-2. 116-63-2 belongs to naphthyridine, auxiliary class Sulfonic acid,Amine,Naphthalene,Alcohol,Organic Pigment, name is 4-Amino-3-hydroxynaphthalene-1-sulfonic acid, and the molecular formula is C10H9NO4S, Quality Control of 116-63-2.
Referemce:
https://en.wikipedia.org/wiki/1,8-Naphthyridine,
1,8-Naphthyridine | C8H6N2 – PubChem