A quantitative analysis of steric and hydrophobic effects in ribonucleoside diphosphate reductase inhibition by thiosemicarbazones.
Ribonucleoside diphosphate reductase (RDR) inhibitory activity of 2-formylpyridine and 1-formylisoquinoline thiosemicarbazones is quantitatively analysed in relation to a steric parameter (van der Waals volume, VW) and the hydrophobic parameter logP. The activity is found to be significantly correlated with VW and very poorly with logP. On the basis of this, it is inferred that RDR inhibition by thiosemicarbazones is very sensitive to steric effects and is little influenced by the hydrophobic character of the molecules.
D055598:Chemical Phenomena; D002627:Chemistry, Physical; D012262:Ribonucleoside Diphosphate Reductase / Q000037:antagonists & inhibitors*; D012264:Ribonucleotide Reductases / Q000037:antagonists & inhibitors*; D013237:Stereoisomerism; D013329:Structure-Activity Relationship; D013882:Thiosemicarbazones / Q000494:pharmacology*
D013882:Thiosemicarbazones; D012264:Ribonucleotide Reductases; D012262:Ribonucleoside Diphosphate Reductase