Original Articles

Bleomycin A derivative, 99mTc-BLAIDA: synthesis and distribution in tumor-bearing mice (author's transl)

Authors: Yu–lin Hu, Yu-yuan Xie, Zheng-qin Tao, Zhen-jia Chen, Jian-shi Zhang, Guang-sheng Ding, De-hua Ye, Yun Wang, Ji-xiao Ma

Abstract

N-(4-bromoacetylaminoace-tanilido) iminodiacetic acid (AIDA) was synthesized by condensation of p-nitroaniline with nitrilotriacetic acid, catalytic reduction and subsequent acylation with bromoacetyl bromide. AIDA was conjugated with cobalt-bleomycin A5 to give BLAIDA, which was in turn labeled with 99mTc to yield 99mTc-BLAIDA.
99mTc-BLAIDA was tested on mice bearing sarcoma 180, brain tumor-22, murine hepatoma or Lewis lung carcinoma. The radioactivities in tumors were much higher than those in blood and other organs. The tumor/organ ratio was highest in case of sarcoma 180 at 12 h after iv 99mTc—BLAIDA. Hence 99mTc-BLAIDA is a potential tumor localizing agent for clinical diagnosis.
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