设计和合成一种蛙皮素肽偶联的三足膦二硫醚配体拓扑结构，用于稳定 fac-[M(CO)3]+ 核心（M=(99m)Tc 或 Re）。
Design and synthesis of a bombesin peptide-conjugated tripodal phosphino dithioether ligand topology for the stabilization of the fac-[M(CO)3]+ core (M=(99 m)Tc or Re).
机构信息
Department of Radiology, University of Missouri, Columbia, Missouri 65211, USA.
出版信息
Inorg Chem. 2011 Jul 4;50(13):6210-9. doi: 10.1021/ic200491z. Epub 2011 May 18.
Abstract
A new tumor-seeking tridentate topology consisting of a phosphino dithioether ((HOCH(2))(2)PCH(2)CH(2)S(CH(2))(n)CH(2)SR; PS(2)) ligand framework for the production of kinetically inert and in vivo stable facial (99m)Tc(CO)(3)(PS(2)) or Re(CO)(3)(PS(2)) is described. The X-ray crystal structure of fac-Re(CO)(3)(PS(2))PF(6) is reported. The bioconjugation strategies for incorporating bombesin (BBN) peptides on to the PS(2) tripodal framework and, thereby, de novo designing of GRP receptor-seeking Tc(PS(2)-BBN)(CO)(3) are developed.
摘要
一种由膦二硫醚（(HOCH(2))(2)PCH(2)CH(2)S(CH(2))(n)CH(2)SR；PS(2))配体框架组成的新型用于生产动力学惰性和体内稳定的面式(99m)Tc(CO)(3)(PS(2))或Re(CO)(3)(PS(2))的肿瘤靶向三齿拓扑结构被描述。报道了 fac-Re(CO)(3)(PS(2))PF(6)的 X 射线晶体结构。设计了将蛙皮素 (BBN) 肽结合到 PS(2)三脚架框架上的生物偶联策略，并在此基础上从头设计 GRP 受体靶向 Tc(PS(2)-BBN)(CO)(3)。
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