5-氟尿嘧啶1-酰氧基甲基衍生物对L1210白血病的抗肿瘤活性。
Antitumor activity of 1-acyloxymethyl derivatives of 5-fluorouracil against L1210 leukemia.
作者信息
Hoshi A, Inomata M, Kanzawa F, Iigo M, Kuretani K
出版信息
J Pharmacobiodyn. 1982 Mar;5(3):208-12. doi: 10.1248/bpb1978.5.208.
Antitumor activity of 15 1-acyloxymethyl derivatives of 5-fluorouracil was examined by both intraperitoneal injection and oral administration in L1210 leukemia system. Therapeutic ratio for dodecanoyloxymethyl derivative by intraperitoneal injection was 23 which was greater than that for 5-fluorouracil (11). On the other hand, undecanoyloxymethyl derivative of 5-fluorouracil showed the highest therapeutic ratio (5.8) when administered orally which was greater than that for 5-fluorouracil (1.9) and 1-(2-tetrahydrofuryl)-5-fluorouracil (1.0).
通过腹腔注射和口服给药两种方式，在L1210白血病系统中检测了15种5-氟尿嘧啶的1-酰氧基甲基衍生物的抗肿瘤活性。十二烷酰氧基甲基衍生物腹腔注射的治疗指数为23，高于5-氟尿嘧啶（11）。另一方面，5-氟尿嘧啶的十一烷酰氧基甲基衍生物口服时治疗指数最高（5.8），高于5-氟尿嘧啶（1.9）和1-(2-四氢呋喃基)-5-氟尿嘧啶（1.0）。
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