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首页> 外文期刊>Japanese Journal of Pharmacology >Antitumor Activity of Two Novel Low Immunosuppressive Fluoropyrimidines UK-21 and UK-25
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Antitumor Activity of Two Novel Low Immunosuppressive Fluoropyrimidines UK-21 and UK-25

机译：两种新型低免疫抑制性氟嘧啶UK-21和UK-25的抗肿瘤活性

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References(7) Cited-By(1) We have previously reported that 2'', 3'', 5''-tris-O-[N-(2-n-propyl-n-pentanoyl)glycyl]-5-fluorouridine (UK-21), a derivative of 5-fluorouridine (5-FUR), and 1-{6-[N-(2-n-propyl-n-pentanoyl)-glycyl]amino-n-hexylcarbamoyl}-5-fluorouracil (UK-25), a derivative of 5-fluorouracil (5-FU), exert their antitumor activity in mice bearing Meth A or EL4 tumor, while their immunosuppressive effects are mild. In the present study, we examined the effects of these compounds on Sarcoma-180 (S-180), P388, L1210, and Lewis lung carcinoma (LLC) in mice by p.o. administration and on Meth A tumor by i.p.-administration. UK-21 given p.o. showed an antitumor effect against S-180, but it showed virtually no antitumor effects against P388, L1210 and LLC. UK-21 given i.p., on the other hand, strongly inhibited the growth of Meth A tumor at a far lower dose than that for oral administration. The bioavailability of UK-21 given p.o. was suspected to be poor. UK-25 given p.o., in contrast, showed the antitumor effect on all of the tumors employed. The bioavailability of UK-25 given p.o. seemed to be comparable to those of other drugs. These results suggest that UK-21 has the potential for development as a parenterally applicable anticancer drug, and UK-25 has the potential as an oral one.
机译：参考文献（7）By-By（1）我们以前曾报道过2''，3''，5''-tris-O- [N-（2-n-丙基-n-戊戊酰基）甘氨酰基] -5-氟尿苷（UK-21），5-氟尿苷（5-FUR）和1- {6- [N-（2-（n-丙基-正戊基戊酰基）-甘氨酰]氨基-正己基氨基甲酰基）-5的衍生物-氟尿嘧啶（5-FU）的衍生物-氟尿嘧啶（UK-25）在患有Meth A或EL4肿瘤的小鼠中发挥其抗肿瘤活性，而其免疫抑制作用则较轻。在本研究中，我们通过p.o检查了这些化合物对小鼠肉瘤180（S-180），P388，L1210和Lewis肺癌（LLC）的影响。腹膜内给药和对甲硫磷进行肿瘤治疗。英国21点点对S-180具有抗肿瘤作用，但对P388，L1210和LLC几乎没有抗肿瘤作用。另一方面，UK-21经腹膜内给药以比口服给药低得多的剂量强烈抑制了Meth A肿瘤的生长。给予p.o. UK-21的生物利用度。被怀疑是穷人。相比之下，UK-25 p.o.表现出对所有使用的肿瘤的抗肿瘤作用。给予p.o.UK-25的生物利用度。似乎可以与其他药物媲美。这些结果表明，UK-21具有作为肠胃外适用的抗癌药的潜力，而UK-25具有作为口服剂的潜力。

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