Synthesis and biological evaluation of amide derivatives of diflunisal as potential anti-tumor agents.
To discover the new medicinal activity, the structure of diflunisal has been modified. Forty amide derivatives of diflunisal were synthesized starting from diflunisal in three steps. Their inhibition growth rate of human lung cancer cell (A549) and human endometrial adenocarcinoma cell (Ishikawa) in vitro was evaluated. The preliminary assay results showed that compounds 6j, 7o and 8c exhibited good anti-tumor activities and excellent selectivity for the Ishikawa cell, may be potential anti-tumor agents.
Zhong
Guang-Xiang
GX
College of Pharmaceutical Science, Zhejiang University of Technology, Hangzhou 310032, PR China. drzhonggx@sohu.com
Chen
Lu-Lu
LL
Li
Hai-Bo
HB
Liu
Fu-Jin
FJ
Hu
Jin-Qing
JQ
Hu
Wei-Xiao
WX
D000577:Amides / Q000737:chemistry*; D000890:Anti-Infective Agents / Q000138:chemical synthesis / Q000494:pharmacology; D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000494:pharmacology*; D045744:Cell Line, Tumor; D002626:Chemistry, Pharmaceutical / Q000379:methods*; D018360:Crystallography, X-Ray / Q000379:methods; D004061:Diflunisal / Q000031:analogs & derivatives* / Q000138:chemical synthesis* / Q000494:pharmacology; D015195:Drug Design; D006801:Humans; D020128:Inhibitory Concentration 50; D008956:Models, Chemical; D015394:Molecular Structure; D009369:Neoplasms / Q000188:drug therapy*
D000577:Amides; D000890:Anti-Infective Agents; D000970:Antineoplastic Agents; D004061:Diflunisal