title: Synthesis of 11C-labeled Kendine 91, a histone deacetylase inhibitor.
abstract: 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.
authors.affiliation: Departamento de Química Orgánica I, Facultad de Química, Universidad del País Vasco--Euskal Herriko Unibertsitatea, Edificio Joxe Mari Korta, Sebastián, Spain.
authors.forename: Maialen
authors.initials: M
authors.lastname: Aginagalde
authors.forename: Vanessa
authors.initials: V
authors.lastname: Gómez-Vallejo
authors.forename: Yosu
authors.initials: Y
authors.lastname: Vara
authors.forename: Fernando P
authors.initials: FP
authors.lastname: Cossío
authors.forename: Jordi
authors.initials: J
authors.lastname: Llop
mesh_terms: D002250:Carbon Radioisotopes / Q000737:chemistry*; D002853:Chromatography, Liquid; D056572:Histone Deacetylase Inhibitors / Q000138:chemical synthesis*; D006877:Hydroxamic Acids / Q000138:chemical synthesis*; D009682:Magnetic Resonance Spectroscopy; D011758:Pyrroles / Q000138:chemical synthesis*
chemical_list: D002250:Carbon Radioisotopes; D056572:Histone Deacetylase Inhibitors; D006877:Hydroxamic Acids; D011758:Pyrroles; C540813:kendine 91