Penetration of Brain and Brain Tumor by Aromatic Compounds as a Function of Molecular Substituents. III

Authors:   A. Soloway,B. Whitman,J. Messer,
Journal: Journal of Medicinal and Pharmaceutical Chemistry
https://doi.org/10.1021/jm01236a018
Abstract: To a great extent there is a correlation between high aqueous/lipid solvent partition coefficients of a series of substituted aromatic boronic acids and the high tumor/brain ratios of these compounds in mice with subcutaneously transplanted gliomas. There are, however, exceptions to this observation and the mechanism of transport into the central nervous system of compounds with low lipid solubility remains obscure. The position of groups on an aromatic nucleus is of importance in determining the degree of penetration of brain. An attempt is made to correlate chemical and physical properties with biologic attributes. © 1962, American Chemical Society. All rights reserved.