Influence of structural and electronic properties of uranyl derivatives on the inhibition of thymidine phosphorylase

Journal Article · Tue Jul 01 00:00:00 EDT 1986 · Pharmaceut. Chem. J.; (United States)

OSTI ID:6899208

Dimoglo, A S; Bersuker, I B; Gorbachev, M Yu

The inhibition of enzymes by definite compounds lies at the basis of the mechanism of the action of most drugs. Uracil and its derivatives are effective inhibitors of thymidine phosphorylase and other related enzymes. Cancer cells are especially sensitive to the absence of thymidine. The study of the inhibiting action of uracil derivatives has been conducted previously. In this article, the authors used the hydrophobicity constants of the substituents, directly bonded to the uracil framework in the 1- and 3-positions and the 6-position as well as the constants of ortho- and meta-substituents in benzene rings bonded to uracil in the investigated compounds for the derivation of correlation equations relating the inhibiting activity to the physicochemical parameters. A table is presented of the 142 uracil derivatives taken for logical-structural analysis.

• Research Organization: Institute of Chemistry, Academy of Sciences of the Moldavian SSR, Kishinev
• OSTI ID: 6899208
• Journal Information: Pharmaceut. Chem. J.; (United States), Vol. 19:9
• Country of Publication: United States
• Language: English

Related Subjects

59 BASIC BIOLOGICAL SCIENCES
ENZYME INHIBITORS
BIOLOGICAL EFFECTS
STRUCTURAL CHEMICAL ANALYSIS
PHOSPHOTRANSFERASES
ENZYME ACTIVITY
THYMIDINE
URANYL COMPOUNDS
BIOCHEMISTRY
CHEMICAL COMPOSITION
COMPUTERIZED SIMULATION
ELECTRONIC STRUCTURE
ESCHERICHIA COLI
INHIBITION
URACILS
ACTINIDE COMPOUNDS
AZINES
BACTERIA
CHEMISTRY
ENZYMES
HETEROCYCLIC COMPOUNDS
HYDROXY COMPOUNDS
MICROORGANISMS
NUCLEOSIDES
NUCLEOTIDES
ORGANIC COMPOUNDS
ORGANIC NITROGEN COMPOUNDS
PHOSPHORUS-GROUP TRANSFERASES
PYRIMIDINES
RIBOSIDES
SIMULATION
TRANSFERASES
URANIUM COMPOUNDS
550200* - Biochemistry