%0 Journal Article
%T Anti-Cancer Activity and Molecular  Docking of Some Pyrano[3,2‑c]quinoline Analogues
%A Abdeltawab M. Saeed
%A Ibrahim M. Abdou
%A Alaa A. Salem
%A Mohammad A. Ghattas
%A Noor Atatreh
%A Shaikha S. AlNeyadi
%J Open Journal of Medicinal Chemistry
%P 1-14
%@ 2164-313X
%D 2020
%I Scientific Research Publishing
%R 10.4236/ojmc.2020.101001
%X Quinoline analogues exhibited diversified biological activities depending on the structure type. A number of natural products with pyrano[3,2-c]quinolone structural motifs and patented chromenes were reported as promising cytotoxic agents. A molecular docking study was employed to investigate the binding and functional properties of 3-amino pyranoquinolinone <strong>2a-c</strong> as anti-cancer agents. The three 3-amino pyranoquinolinone <strong>2a-c</strong> showed an interesting ability to intercalate the DNA-topoisomerase complex and were able to obtain energetically favorable binding modes (<span style=\"white-space:nowrap;\"><span style=\"white-space:nowrap;\"><span style=\"white-space:nowrap;\">&amp;#8722;</span></span></span>8.3 - <span style=\"white-space:nowrap;\"><span style=\"white-space:nowrap;\"><span style=\"white-space:nowrap;\">&amp;#8722;</span></span></span>7.5 kcal/mol). Compound <strong>2c</strong> containing butyl chain superiority over the other two compounds <strong>2a-b</strong> which appeared to be involved in arene-H interactions with the two dG13 aromatic centers. The butyl chain also appeared to be immersed into a side subpocket formed by the side chains of Asn520 and Glu522 and the backbone amide of Arg503, Gly504, Lys505 and Ile506. Hence, the 3-amino pyranoquinolinone <strong>2c</strong> used as starting material to prepare derivatives of pyrano[3,2-c]quinolone containing 1,2,4-triazine ring <strong>4a-b</strong> which will enhance the anti-cancer activity. Pyrano[3,2-<em>c</em>]quinoline-2,5-diones <strong>2a-c</strong> and <strong>4a-b</strong> were evaluated <em>in vitro</em> on cell lines Ehrlich Ascites carcinoma cells (EAC), liver cancer cell line Hep-G2 and breast cancer cell line MCF-7 for the development of novel anticancer agents. The screening results revealed that compounds <strong>4a-b</strong> were found most active candidates as anticancer agents.
%K Pyrano[3
%K 2-c]quinoline
%K Molecular Docking
%K Anticancer
%U http://www.scirp.org/journal/PaperInformation.aspx?PaperID=98685