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Preparation of Boron-containing Bovine -Globulin as a Model Compound for a New Approach to Slow Neutron Therapy of Tumors¹

Department of Chemistry, University of Pittsburgh, Pittsburgh, Pennsylvania 15213

The N-carboxy anhydride of DL-4-boronophenylalanine was synthesized and used to prepare soluble copoly (DL-alanyl-DL-4-boronophenylalanyl) bovine -globulin. Characterization of the resulting globulin was accomplished by amino acid and elemental analyses. Variations in the ratio of N-carboxy-DL-alanine anhydride to N-carboxy-DL-4-boronophenylalanine anhydride used appeared to affect the solubility of the modified globulins. The maximum boron content of the resulting materials was approximately 36 boron atoms per molecule of protein. This technique, if applied to antitumor antibodies, may provide a means by which ¹⁰B can be localized in neoplasms. Neutron capture therapy could then be attempted.

¹ Support of this research by two Unrestricted Research Grants from the Gulf Oil Foundation and by American Cancer Society Institutional Research Grant IN-58 is gratefully acknowledged.

² The author appreciates summer support by the University of Pittsburgh Medical Alumni Association.

³ To whom correspondence should be addressed.

Received 2/28/72. Accepted 6/ 2/72.