Synthesis and biological activity of 125I/127I-phenylboronic acid derivatives.

B M Kinsey, A I Kassis

Index: Nucl. Med. Biol. 20(1) , 13-22, (1993)

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Abstract

Three iodinated phenylboronic acids have been synthesized: 4-iodophenylboronic acid (2a), 3-(4-iodobenzenesulfonamido)phenylboronic acid (5a) and 3-(5-dimethylamino-6-iodo-1-naphthalenesulfonamido)phenylboronic acid (6a). The corresponding no-carrier-added 125I derivatives 2b, 5b and 6b have been prepared in good yield by selective displacement of the tributylstannyl group. Compound 6b was concentrated in vitro preferentially in HT-29 human colon carcinoma cells compared to V79 Chinese hamster lung fibroblasts and showed selective retention in PaCa-2 human pancreatic cancer cells grown as solid tumor xenografts in the nude mouse.