金属有机小分子激酶抑制剂-奥帕尼布®中 Re 和 99mTc 的直接掺入。
Organometallic small molecule kinase inhibitors - direct incorporation of Re and 99mTc into Opaganib®.
机构信息
University of Zurich, Department of Chemistry, Zurich, Switzerland.
Chimie ParisTech, PSL University, CNRS, Institute of Chemistry for Life and Health Sciences, Laboratory for Inorganic Chemical Biology, Paris F-75005, France.
出版信息
Chem Commun (Camb). 2021 Dec 9;57(98):13349-13352. doi: 10.1039/d1cc03678e.
[(η5-Cp)Re(CO)] was incorporated into the kinase inhibitor Opaganib®. The resulting bioorganometallic complex showed a similar anti-cancer activity to Opaganib® against PC-3 cancer cells. The IC value for the kinase SK2 is 30x higher than that of Opaganib®. The 99mTc homologue was synthesized, completing a matched-pair for molecular theranostics.
[(η5-Cp)Re(CO)] 被整合到激酶抑制剂 Opaganib®中。所得的生物有机金属配合物对 PC-3 癌细胞表现出与 Opaganib®相似的抗癌活性。激酶 SK2 的 IC 值比 Opaganib®高出 30 倍。99mTc 类似物已被合成，完成了分子治疗学的配对。
Zotero 插件