Synthesis and Cytotoxic Evaluation of Substituted Sulfonyl-N-hydroxyguanidine Derivatives as Potential Antitumor Agents
作者： Ji-Wang Chern , Yu-Ling Leu , Shan-Shue Wang , Ruwen Jou , Chin-Fen Lee
DOI: 10.1021/JM9607818
关键词: Chemical synthesis 、 Cytotoxicity 、 Lead compound 、 In vitro 、 Moiety 、 Sulfonyl 、 Aromaticity 、 Cytotoxic T cell 、 Stereochemistry 、 Chemistry
摘要: A series of sulfonyl-N-hydroxyguanidine derivatives was designed and synthesized for cytotoxic evaluation as potential anticancer agents on the basis lead compound LY-181984. Replacement ureido moiety with hydroxyguanidine provided a stable agent. The conformation derivatives, such N-(4-chlorophenyl)-N‘-[(benzo[2,1,3]thiadiazol-4-yl)sulfonyl]-N‘‘-hydroxyguanidine (4g), investigated utilizing HMBC NMR, theoretical calculations, X-ray crystallography, indicated stacking two aromatic rings. were evaluated in vitro cytoxicity against five human tumor cell lines, including HepG2, TSGH 8302, COLO 205, KB, MOLT-4. activities derived compounds lines equal to or greater than that compound. N-(4-Chlorophenyl)-N‘-[[3,5-dichloro-4-(4-nitrophenoxy)phenyl]sulfonyl]-N‘‘-hydroxyguanidine (4n) N-(4-chlorophenyl)-N‘-[[3,5-dichloro-4-(2-chlor...
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