| 摘要 |
<p>Anticancer compsn. comprises 5-fluorouracil (I) or a cpd. (II) capable of producing (I) in vivo together with a pyridine deriv. of formula (III). In (III) R1 = OH or acyloxy; R2, R4 = H, halogen, NH2, COOH, CONH2, CN, NO2, 1-6C alkyl, 2-6C alkenyl or (1-6C)alkoxycarbonyl; R3, R5 = H, OH or acyloxy. When at least one of R1, R3 and R5 = OH, then the 1-posn. of the (III) ring may have the -NH- structure by keto-enol tautomerism, and this H atom may be replaced by 1-6C alkyl, tetrahydrofuranyl, tetrahydropyranyl, (1-6C) alkoxy-(1-6C)alkyl, phthalidyl, CONH2, (1-6C)alkoxycarbonyl-(1-6C)alkylcarbamoyl, Ph-(1-6C)alkoxy-(1-6C)alkyl, phenylcarbamoyl (itself opt. ring substd.), (1-6C)alkylcarbamoyl, COOH-(1-6C)alkylcarbamoyl, (1-6C)alkylthio-(1-6C)alkyl or 2-6C alkenyl. Provided that (III) is not a cpd. of formula (IV), where R = H, 1-6C alkyl, tetrahydrofuranyl, tetrahydropyranyl, (1-6C)alkoxy-(1-6C)alkyl, (1-6C)alkylcarbamoyl, (1-6C)alkylthio-(1-6C)alkyl or 2-6C alkenyl.</p> |
