Xavier, Catarina published the artcileSynthesis, characterization, and evaluation of a novel 99mTc(CO)3 pyrazolyl conjugate of a peptide nucleic acid sequence, Quality Control of 186046-83-3, the publication is JBIC, Journal of Biological Inorganic Chemistry (2008), 13(8), 1335-1344, database is CAplus and MEDLINE.
The 16-mer peptide nucleic acid sequence H-A GAT CAT GCC CGG CAT-Lys-NH2 (1), which is complementary to the translation start region of the N-myc oncogene mRNA, was synthesized and conjugated to a pyrazolyl diamine bifunctional chelator (pz). The novel conjugate pz-A GAT CAT GCC CGG CAT-Lys-NH2 (2) was labeled with technetium tricarbonyl, yielding quant. the complex fac-[99mTc(CO)3(κ3-pz-A GAT CAT GCC CGG CAT-Lys-NH2)]2+ (4). Complex 4 was obtained with high radiochem. purity and high specific activity, revealing high stability in human serum and in cell culture medium. The identity of 4 was confirmed by comparing its reversed-phase high performance liquid chromatog. profile with that of the rhenium analog fac-[Re(CO)3(κ3-pz-A GAT CAT GCC CGG CAT-Lys-NH2)]2+ (3), prepared by conjugation of fac-[Re(CO)3(3,5-Me2pz(CH2)2N((CH2)3COOH)(CH2)2NH2)]+ to 1, using solid-phase techniques. UV melting experiments of 1 and 3 with the complementary DNA sequence led to the formation of stable duplexes, indicating that the conjugation of 1 to the pyrazolyl chelator and to the metal fragment fac-[M(CO)3]+ did not affect the recognition of the complementary sequence as well as the duplex stability. For a first screening, SH-SY5Y human neuroblastoma cells, which express N-myc, were treated with 4. The results show that 4 internalizes (7% of the activity goes into the cells, after 4 h at 37°), presenting also a relatively high cellular retention (only 40% of internalized activity is released from the cells after 5 h).
JBIC, Journal of Biological Inorganic Chemistry published new progress about 186046-83-3. 186046-83-3 belongs to amides-buliding-blocks, auxiliary class Purine,Carboxylic acid,Amine,Benzene,Amide,Others,PNA,, name is 2-(N-(2-((((9H-Fluoren-9-yl)methoxy)carbonyl)amino)ethyl)-2-(2-(((benzhydryloxy)carbonyl)amino)-6-oxo-5H-purin-9(6H)-yl)acetamido)acetic acid, and the molecular formula is C2H3N3, Quality Control of 186046-83-3.
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