High Cytotoxic Effect by Combining Copper-64 with a NOTA-Terpyridine Platinum Conjugate

Khosravifarsani Meysam; Ait-Mohand Samia; Paquette Benoit; Sanche Leon; Guerin Brigitte

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High Cytotoxic Effect by Combining Copper-64 with a NOTA-Terpyridine Platinum Conjugate

机译：通过将铜-64与Nota-Terpyridine铂共轭结合，通过结合高细胞毒性效果

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Terpyridine platinum (TP)-based chemotherapeutic agents target three-dimensional structures on DNA known as G-quadruplexes. We report the rational design and synthesis of a TP conjugate combined with copper-64 (Cu-64), the decay characteristics of which include emission of beta(-) and Auger electrons for radiotherapy and beta(+) particles for positron emission tomography (PET) imaging. The present experimental studies show that the novel [Cu-64]Cu-1,4,7-triazacyclononane-1,4,7-triacetic acid (NOTA)-TP is stable, permitting selective killing of cancer cells. The antitumor activity of [Cu-64]Cu-NOTA-TP at high apparent molar activity is in the low nanomolar range and 27,800-fold greater than that of Cu-nat-NOTA-TP at 24 h post treatment. These results suggest that this combination of a cytotoxic TP agent with Cu-64 has considerable potential for cancer treatment and PET imaging.

机译：基于三联吡啶铂（TP）的化疗药物靶向DNA上的三维结构，称为G-四链体。我们报道了一种结合铜-64（Cu-64）的TP结合物的合理设计和合成，其衰减特性包括放射治疗用β（-）和俄歇电子的发射，以及正电子发射断层扫描（PET）成像用β（+）粒子的发射。目前的实验研究表明，新型[Cu-64]Cu-1,4,7-三氮杂环壬烷-1,4,7-三乙酸（NOTA）-TP是稳定的，允许选择性杀伤癌细胞。[Cu-64]Cu-NOTA-TP在高表观摩尔活性下的抗肿瘤活性在低纳摩尔范围内，并且在治疗后24小时比Cu-nat-NOTA-TP高27800倍。这些结果表明，细胞毒性TP试剂与Cu-64的组合在癌症治疗和PET成像方面具有相当大的潜力。

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《Journal of Medicinal Chemistry》 |2021年第10期|共12页
作者
Khosravifarsani Meysam; Ait-Mohand Samia; Paquette Benoit; Sanche Leon; Guerin Brigitte;
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Univ Sherbrooke Fac Med &

Hlth Sci Dept Nucl Med &

Radiobiol Sherbrooke PQ J1H 5N4 Canada;

Univ Sherbrooke Fac Med &

Hlth Sci Dept Nucl Med &

Radiobiol Sherbrooke PQ J1H 5N4 Canada;

Univ Sherbrooke Fac Med &

Hlth Sci Dept Nucl Med &

Radiobiol Sherbrooke PQ J1H 5N4 Canada;

Univ Sherbrooke Fac Med &

Hlth Sci Dept Nucl Med &

Radiobiol Sherbrooke PQ J1H 5N4 Canada;

Univ Sherbrooke Fac Med &

Hlth Sci Dept Nucl Med &

Radiobiol Sherbrooke PQ J1H 5N4 Canada;

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正文语种 eng
中图分类药学;
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High Cytotoxic Effect by Combining Copper-64 with a NOTA-Terpyridine Platinum Conjugate

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