A highly effective bifunctional ligand for radioimmunotherapy applications

Hyun-Soon Chong; Hyun A. Song; Chi Soo Kang; Thien Le; Xiang Sun; Mamta Dadwal; Hyunbeom Lee; Xiaoli Lan; Yunwei Chen; Anzhi Dai

doi:10.1039/C0CC05707J

A highly effective bifunctional ligand for radioimmunotherapy applications†

Hyun-Soon Chong,*^a Hyun A. Song,^a Chi Soo Kang,^a Thien Le,^a Xiang Sun,^a Mamta Dadwal,^a Hyunbeom Lee,^a Xiaoli Lan,^a Yunwei Chen^a and Anzhi Dai^a

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^a Chemistry Division, Biological, Chemical, and Physical Sciences Department, Illinois Institute of Technology, 3101 S. Dearborn St, LS 182, Chicago, USA
E-mail: chong@iit.edu
Fax: 312-567-3494
Tel: 312-567-3235

Abstract

A novel bifunctional ligand (3p-C-NETA) for antibody-targeted radioimmunotherapy (RIT) of β-emitting radioisotopes ⁹⁰Y and ¹⁷⁷Lu was efficiently synthesized via an unexpected regiospecific ring opening of an aziridinium ion. 3p-C-NETA instantly formed a very stable complex with ⁹⁰Y or ¹⁷⁷Lu. 3p-C-NETA is an excellent bifunctional ligand for RIT.

Chemical Communications

A highly effective bifunctional ligand for radioimmunotherapy applications†

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A highly effective bifunctional ligand for radioimmunotherapy applications

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