Cyanopyrazoles as analogs of purine precursors--I. Inhibitory effect on purine biosynthesis de novo.
作者信息
Spassova M K, Grancharov K C, Golovinsky E V
出版信息
Int J Biochem. 1984;16(10):1091-4. doi: 10.1016/0020-711x(84)90094-6.
PMID:6519347
Abstract
The in vitro inhibition of purine biosynthesis de novo by a series of cyanopyrazoles was studied. At concentration 1 mM trichloromethyl analogs (3(5)-amino-4-cyano-5(3)-trichloromethylpyrazole and N-hydroxyethyl-3(5)-amino-4-cyano-5(3)-trichloromethylpyrazole) were found to inhibit IMP synthesis 80 and 30% respectively. GAR synthesis was inhibited at a lower degree at the same range of concentrations. The compounds demonstrated a similar pattern of inhibition of the last steps, e.g. AICAR formylation and cyclization as found on the whole pathway.
摘要
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