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巴比土酸衍生物罕见有抗瘤活性,但由加拿大合成的Merbarone(NSC-336628)是硫代巴比土酸与苯胺的酰胺键合物。经研究证实,它对腹腔接种的L 1210小鼠白血病(每日100mg/kg腹腔注射1～9天)至少50%有治愈作用(30天无明显的肿瘤生长),中数生命延长率至少为200%。皮下接种疗效相似,提示具全身性作用。但大脑内接种无效,这可能为在生理pH(酸性pka)下与该药的离子化作用有关。皮下接种L 1210小鼠每日腹腔或口服给药连续5～9天疗效最好,间歇腹腔注射或1次静注给药均无效,
Barbiturates are rare of antitumor activity, but Merbarone (NSC-336628) synthesized in Canada is an amide bond of thiobarbituric acid with aniline. The study confirmed that it has a healing effect on at least 50% of intraperitoneal L 1210 mouse leukemia (1 to 9 days per 100 mg / kg intraperitoneal injection) (no significant tumor growth for 30 days), and the median prolongation of life is at least 200%. Subcutaneous vaccination similar efficacy, suggesting a systemic effect. However, intracerebral inoculation is ineffective, which may be related to the drug’s ionization at physiological pH (acidic pka). Subcutaneously inoculated L1210 mice daily intraperitoneal or oral administration of 5 to 9 consecutive days the best effect, intermittent intraperitoneal injection or 1 intravenous administration are not effective,