In contrast intratumoral application of A8 plus 4 X 10(12)n/cm2 neutrons gave a growth delay of 7-14 days the fraction of (G2 + M) cells rose from 35% (neutrons alone) to 52%, as evaluated from flow cytometry. plus 5 X 10(12)n/cm2 resulted in a growth delay of 3-6 days. The neutrons are almost exclusively absorbed by boron-10. Application of the boron 10 glycine-amide analog A8 i.p. Boron-10 is administered to the cancerous cells and then the body is bombarded with slow neutrons. 771 produced a tumor growth delay of 1-2 days for tumor volume doubling. Application of A8 alone (0.4 mg/g i.p.) or thermal neutron irradiation of the tumor EO. In addition, boron-10 concentration in the tumor were analyzed with prompt gamma-activation analysis and neutron capture radiography (Kodak-Pathé LR 115) at the MRR reactor in Brookhaven after i.p. The disclosed method includes making a starting target from a substance which contains a mixture of boron-10 and boron-11 isotopes, irradiating the target with neutron flux to the required or. Boron distribution between tumor and muscle was analyzed by emission spectroscopy with inductively coupled plasma (ICP) following injection of a suspension of peanut oil emulsion. The effects of this compound were tested on the syngeneic solid adenocarcinoma EO 771 on the right hind leg of male C57 BL/6J mice under standard conditions, by measuring tumor volume growth delay and cell cycle changes using flow cytometry. Now the boron-10 glycineamide analog (A8), amineboryl-carboxamide has been synthesized it contains 13.81% boron (90% Boron 10 + 10% Boron 11) and shows a very low toxicity in mice. Neutron capture therapy with two boron-10 amino acid analogs of low toxicity has been tested in recent years: (a) trimethylamine-carboxyborane, (A3) and (b) amine-carboxyborane, (A7). If a tumor can be preferentially loaded with a suitable boron-10 compound and irradiated with thermal neutrons, malignant cells can be selectively destroyed via the alpha-particle + Li 7-nucleus from the reaction 10B(n, alpha)7Li.
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