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oai:ojs.www.eurjchem.com:article/1318 2015-12-31T11:02:45Z eurjchem:ART driver

New N(4)-methylthiosemicarbazone derivatives: Synthesis, characterization, structural properties, DNA interactions and antiproliferative activity Hussein, Mouayed Guan, Teoh Siang DNA binding Electronic transitions X-ray crystal structure Fluorescence emissions Antiproliferative activity N(4)-Methylthiosemicarbazone Five new thiosemicarbazone compounds derived from N(4)-methylthiosemicarbazide and 5-bromo-2-hydroxybenzaldehyde (1), 2,4-dihydroxybenzaldehyde (2), 3-ethoxy-2-hydroxy benzaldehyde (3), 3-tert-butyl-2-hydroxybenzaldehyde (4), and 2-acetylpyridine (5) have been synthesized. The molecular structures of the prepared compounds were identified using by single crystal X-ray crystallography. The binding properties of the compounds with calf thymus DNA were analyzed by UV, fluorescence titration, and viscosity measurements. The cytotoxic properties of the compounds were tested against human colorectal cell lines (HCT 116). The compounds showed greater pronounced activity than the standard reference drug 5-fluorouracil (IC50 = 7.3 μM). The results showed that the activity strength of these compounds depends on the lipophilic properties that provided by the terminal N(4)-substituent and aromatic ring-substituent, as well as the planarity that provided by the geometrical and conformational structures of the compounds. Atlanta Publishing House LLC 2015-12-31 info:eu-repo/semantics/article info:eu-repo/semantics/publishedVersion application/pdf text/plain text/plain text/plain text/plain text/plain https://www.eurjchem.com/index.php/eurjchem/article/view/1318 10.5155/eurjchem.6.4.451-460.1318 European Journal of Chemistry; Vol. 6 No. 4 (2015): December 2015; 451-460 2153-2257 2153-2249 eng https://www.eurjchem.com/index.php/eurjchem/article/view/1318/pdf_1318 https://www.eurjchem.com/index.php/eurjchem/article/view/1318/2575 https://www.eurjchem.com/index.php/eurjchem/article/view/1318/2576 https://www.eurjchem.com/index.php/eurjchem/article/view/1318/2577 https://www.eurjchem.com/index.php/eurjchem/article/view/1318/2578 https://www.eurjchem.com/index.php/eurjchem/article/view/1318/2579