Peindy N’Dongo, Harmel W.’s team published research in Nuclear Medicine and Biology in 2010-04-30 | CAS: 1205-72-7

Nuclear Medicine and Biology published new progress about Melanoma. 1205-72-7 belongs to class piperidines, name is 1-Benzylpiperidin-4-amine dihydrochloride, and the molecular formula is C12H20Cl2N2, Quality Control of 1205-72-7.

Peindy N’Dongo, Harmel W. published the artcilePreparation and biological evaluation of cyclopentadienyl-based 99mTc-complexes [(Cp-R)99mTc(CO)3] mimicking benzamides for malignant melanoma targeting, Quality Control of 1205-72-7, the main research area is cyclopentadienyl technetium 99m complex preparation melanoma imaging.

The biol. evaluation of half-sandwich 99mTc-complexes that surrogate iodobenzamide with a high affinity for melanin tumor tissue is described. We have synthesized via retro Diels-Alder reaction two models of 99mTc complexes which possess the piano stool [Cp99mTc(CO)3] motif instead of a Ph ring as in the original iodobenzamide 123I-N-(N-benzylpiperidin-4-yl)-2-iodobenzamide (2-IBP) and N-(2-diethylaminoethyl)-4-iodobenzamide (BZA). Diels-Alder products 2a-2b (HCp-CONHR)2 (2a, R=2-diethylaminoethyl; 2b, R=benzylpiperidin-4-yl) were prepared and reacted with fac-[99mTc(H2O)3(CO)3]+ 1 in water to produce the corresponding 99mTc complexes [(2a)99mTc(CO)3] 4a and [(2b)99mTc(CO)3] 4b. The structures of the 99mTc complexes on the no-carrier-added level have been confirmed by chromatog. comparison with the corresponding rhenium complexes and, macroscopically characterized by IR, NMR, ESI-MS and X-ray crystallog. for [triclinic, P-1, a=7.3518(1) Å, b=8.0309(2) Å, c=17.5536(3) Å, α=99.1260(5)°, β=90.4215(14)°, γ=117.0187(11)°]. The radioconjugate showed good in vitro stability. In murine melanoma B16F1 cells, significant cellular uptake (43.9% of the total applied activity) was attained after 4 h at 37°C with about 50% of the cell-associated radioactivity being internalized in the cells (22% of the applied activity). Furthermore, in melanoma-bearing C57BL6 mice, tumor uptake values of 3.39±0.50 %ID g-1 and 3.21±0.26 %ID g-1 at 1 and 4 h postinjection, resp., were observed indicating a good retention of in the tumor.

Nuclear Medicine and Biology published new progress about Melanoma. 1205-72-7 belongs to class piperidines, name is 1-Benzylpiperidin-4-amine dihydrochloride, and the molecular formula is C12H20Cl2N2, Quality Control of 1205-72-7.

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem