Synthesis of novel quinoxaline derivatives and its cytotoxic activities.
Substituted dihydroquinozalin-2-ones (1-16) have been synthesized easily by the use of copper-catalyzed coupling method. The reactions of 2-haloanilines with a variety of alpha-amino acids in the presence of copper (I) iodide gave corresponding 3-substituted dihydroquinozalin-2-ones in up to 86% yield. Some new quinoxalin-2-ones (2, 4, 5, 13 and 16) have moderate cytotoxic activity toward HeLaS3 cell lines at 4.9-18.1microM.
Tanimori
Shinji
S
Department of Bioscience and Informatics, Graduate School of Life and Environmental Sciences, Osaka Prefecture University, 1-1 Gakuencho, Nakaku, Sakai, Osaka 599-8531, Japan. tanimori@bioinfo.osakafu-u-ac.jp
Nishimura
Takeshi
T
Kirihata
Mitsunori
M
D000596:Amino Acids / Q000737:chemistry; D000814:Aniline Compounds / Q000737:chemistry; D002384:Catalysis; D002626:Chemistry, Pharmaceutical / Q000379:methods; D003300:Copper / Q000737:chemistry; D015195:Drug Design; D006367:HeLa Cells; D006801:Humans; D020128:Inhibitory Concentration 50; D008956:Models, Chemical; D015394:Molecular Structure; D011810:Quinoxalines / Q000138:chemical synthesis* / Q000494:pharmacology; D012997:Solvents / Q000737:chemistry; D013696:Temperature
D000596:Amino Acids; D000814:Aniline Compounds; D011810:Quinoxalines; D012997:Solvents; D003300:Copper; C023650:aniline