POTENTIAL ANTICANCER AGENTS .5. SYNTHESIS AND BIOCHEMICAL STUDIES OF 5-FLUORINATED PYRIMIDINE-6-CARBOXALDEHYDES AND DERIVATIVES

被引：38

作者：

PIANTADO.C

KIM, CS

IRVIN, JL

机构：

[1] The Departments of Medicinal Chemistry and Biochemistry, University of North Carolina, Chapel Hill, North Carolina

来源：

JOURNAL OF PHARMACEUTICAL SCIENCES | 1969年 / 58卷 / 07期

关键词：

5‐Fluorinated pyrimidine‐6‐carboxaldehydes; derivatives–synthesis; Anticancer screening–5‐fluorinated pyrimidine‐6‐carboxaldehydes; Cell suspensions–respiration; glycolysis determinations; Nucleic acid biosynthesis–inhibition;

D O I：

10.1002/jps.2600580704

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A series of 5‐fluoropyrimidine‐6‐carboxaldehydes with varying 2‐substituents was prepared from which a number of 6‐ substituted 5‐fluoropyrimidines were derived. Several compounds in this series were found to inhibit growth of the Ehrlich ascites carcinoma only slightly less effectively than 5‐fluorouracil and the strongest inhibition of the series was 2‐ethylthio‐5‐fluoropy‐ rimidine‐6‐carboxaldehyde, I‐8. The replacement of the formyl group by other substituents tended to decrease or to abolish the inhibitory activity. The various compounds in this series inhibit respiration and glycolysis of Ehrlich ascites carcinoma cells, but these inhibitory effects were obtained only at concentrations which were several fold higher than those required for inhibition of nucleic acid synthesis as reported previously. Copyright © 1969 Wiley‐Liss, Inc., A Wiley Company

引用

页码：821 / &