5-氟尿嘧啶衍生物。XXII。1-氨基甲酰基-5-氟尿嘧啶的合成与抗肿瘤活性
5-Fluorouracil derivatives. XXII. Synthesis and antitumor activities of 1-carbamoyl-5-fluorouracils.
作者信息
Ozaki S, Kong X, Watanabe Y, Hoshiko T, Koga T, Ogasawara T, Takizawa T, Fujisawa H, Iigo M, Hoshi A
机构信息
Department of Chemistry, Shandong University, Jinan, China.
出版信息
Chem Pharm Bull (Tokyo). 1997 Aug;45(8):1372-5. doi: 10.1248/cpb.45.1372.
PMID:9301037
Abstract
Fifty-four 1-carbamoyl-5-fluorouracils were synthesized from 5-fluorouracil and isocyanate or amine. Antitumor activity was tested in the L-1210 tumor system, and 11 compounds gave better values of therapeutic ratio than HCFU (1-hexylcarbamoyl-5-fluorouracil). 1-(4-Methoxycyclohexylcarbamoyl)-5-fluorouracil gave the best result.
摘要
由5-氟尿嘧啶与异氰酸酯或胺合成了54种1-氨甲酰基-5-氟尿嘧啶。在L-1210肿瘤系统中测试了其抗肿瘤活性，有11种化合物的治疗指数值优于HCFU（1-己基氨甲酰基-5-氟尿嘧啶）。1-(4-甲氧基环己基氨甲酰基)-5-氟尿嘧啶的效果最佳。
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