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제109회 대한화학회 학술발표회, 총회 및 기기전시회 안내 New derivatives of TE2A with enhanced stability for Cu(II) ions; a better option for TE2A as a bifunctional chelator

2012년 2월 22일 15시 49분 18초
INOR.P-249 이곳을 클릭하시면 발표코드에 대한 설명을 보실 수 있습니다.
4월 25일 (수요일) 18:00~21:00
저자 및
AJIT V. DALE, DARPAN N.PANDYA, 김정영1, 이호춘2, 하영수, 김종희, 이웅희, 안광일1, 유정수
경북대학교 의과대학 분자의학교실, Korea
1한국원자력의학원 방사성의약품연구팀, Korea
2대구경북과학기술원 에너지시스템공학, Korea
Importance of bifunctional chelators (BFCs) has increased over last decade, due to their potential application in the field of radiopharmaceuticals. In order to be successful, a BFC should form stable complexes with metal ions. Cyclam with two acetate pendant arms, TE2A was found to be a better chelator for Cu(II) ions than widely used TETA. In order to check the effect of methyl substitutions on two remaining secondary amines of TE2A backbone with respect to their stability with Cu(II) ions, we synthesized mono and di substituted TE2A (MM-TE2A and DM-TE2A) in five and four steps in good overall yield. The Cu(II) complexes of MM/DM-TE2A were synthesized in high yields. Acidic decomplexation and cyclic voltammetry experiments were carried out for Cu(II) complexes to evaluate their kinetic stability. Cu-TE2A was used for the comparison studies. The degradation pattern of Cu(II) complexes was monitored using a HPLC system. Cu-DM-TE2A showed higher stability than Cu-MM-TE2A. Cyclic voltammetry studies showed quasi irreversible reduction potential for both Cu-MM- and Cu-DM-TE2A. MM- and DM-TE2A were quantitatively radiolabeled with 64Cu using 64CuCl2. Both 64Cu-MM/DM-TE2A did not show any sign of decomplexation for up to 24 h in the serum stability test. LogP studies confirmed that 64Cu-DM-TE2A was more lipophilic than 64Cu-MM-TE2A. Biodistribution studies revealed that both 64Cu-MM- and 64Cu-DM-TE2A showed rapid clearance from body. To conclude, methyl substitutions on TE2A on remaining secondary amine of cyclam backbone resulted in more stable Cu(II) complexation than TE2A.