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Molecular Pharmacology, Vol 1, 87-92, Copyright © 1965 by the American Society for Pharmacology and Experimental Therapeutics

The Correlation of Localization Rates of Benzeneboronic Acids in Brain and Tumor Tissue with Substituent Constants

CORWIN HANSCH 1, A. RUTH STEWARD 1, and JUNKICHI IWASA 1

1 Department of Chemistry, Pomona College, Claremont, California

Substituent constants and regression analysis have been used to correlate the localization of substituted benzeneboronic acids in brain and tumor tissue of mice. It is shown that localization in the brain can be rationalized in terms of one parameter, pgr, obtained from octanol: water partition coefficients. Localization in the tumor depends on an additional electronic parameter, dgr. Localization in the boronic acid series is compared with biologic activity in a series of barbituric acids.

Note:
ACKNOWLEDGMENT This work was supported by Research Grant GM-07492 from the National Institutes of Health. We thank Edna W. Deutsch for assistance in the preparation of the manuscript.

Submitted on April 14, 1965






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