Synthesis and bioevaluation of 5-fluorouracil derivatives.
A series of six novel 5-fluorouracil derivatives 1-6 were synthesized and their structures confirmed by (1)H- and (13)C-NMR, MS and elemental analysis. The preliminary in vitro antitumor activities against B16, K562 and CHO cells and the in vivo inhibitions of liver cancer H(22) demonstrated that some of these compounds effectively inhibit the growth of tumor cells, but the in vivo trials in mice revealed that the compounds also exhibited serious liver and lung tissue toxicity. The hydrolysis experiments indicated that this type of compound did not readily liberate 5-fluorouracil, as expected.
School of Pharmaceutical Science and Technology, Tianjin University, 92 Weijin Road, Nankai District, 300072, Tianjin, PR China. tzynew@yahoo.com.cn
Zhi-Yong
ZY
Tian
Gang-Jun
GJ
Du
Song-Qiang
SQ
Xie
Jin
J
Zhao
Wen-Yuan
WY
Gao
Chao-Jie
CJ
Wang
D000818:Animals; D000964:Antimetabolites, Antineoplastic / Q000138:chemical synthesis / Q000737:chemistry / Q000627:therapeutic use; D002460:Cell Line; D045744:Cell Line, Tumor; D004354:Drug Screening Assays, Antitumor; D005472:Fluorouracil / Q000138:chemical synthesis / Q000737:chemistry / Q000627:therapeutic use; D006801:Humans; D008113:Liver Neoplasms / Q000188:drug therapy / Q000378:metabolism; D051379:Mice; D015394:Molecular Structure; D009368:Neoplasm Transplantation
D000964:Antimetabolites, Antineoplastic; D005472:Fluorouracil