Aginagalde Maialen, Gómez-Vallejo Vanessa, Vara Yosu, Cossío Fernando P, Llop Jordi
Departamento de Química Orgánica I, Facultad de Química, Universidad del País Vasco--Euskal Herriko Unibertsitatea, Edificio Joxe Mari Korta, Sebastián, Spain.
Appl Radiat Isot. 2012 Oct;70(10):2552-7. doi: 10.1016/j.apradiso.2012.05.016. Epub 2012 Jun 7.
In the present paper, the synthesis of (11)C-labeled Kendine 91 (a HDAC inhibitor which has shown in vitro and in vivo activity in HCT 116 and MOLT 4 human cancer cell lines) is described for the first time. The radiosynthesis has been approached by reaction of the non-radioactive precursor 6-((3-(4-hydroxyphenyl)-5-phenyl-1H-pyrrole-2-carboxamide))hexanehydroxamic acid with [(11)C]CH(3)I in basic media. Despite the presence of more than one reactive site in the chemical structure of the precursor, acceptable radiochemical yield (8.2±2.1%, decay corrected to the end of bombardment), specific activity (28.2±9.4 GBq/μmol) and radiochemical purity values (>95%) were obtained in reasonably short preparation times (~40 min). Despite the moderate radiochemical yield, final radioactivity and radioactivity concentration values (1.8±0.3 GBq and 180 MBq/ml, respectively) should be sufficient for putative in vivo studies in animals.
在本论文中，首次描述了（11）C标记的肯丁91（一种组蛋白去乙酰化酶抑制剂，已在HCT 116和MOLT 4人癌细胞系中显示出体外和体内活性）的合成。通过非放射性前体6-((3-(4-羟基苯基)-5-苯基-1H-吡咯-2-甲酰胺))己烷异羟肟酸与[(11)C]CH(3)I在碱性介质中的反应进行放射性合成。尽管前体的化学结构中存在多个反应位点，但在相当短的制备时间（约40分钟）内获得了可接受的放射化学产率（8.2±2.1%，校正至轰击结束时的衰变）、比活度（28.2±9.4 GBq/μmol）和放射化学纯度值（>95%）。尽管放射化学产率适中，但最终的放射性和放射性浓度值（分别为1.8±0.3 GBq和180 MBq/ml）应该足以用于动物体内的假定研究。
