176752-35-5Relevant articles and documents
New SIRT2 inhibitors: Histidine-based bleomycin spin-off
Ali, Taha F.S.,Ciftci, Halil I.,Radwan, Mohamed O.,Koga, Ryoko,Ohsugi, Takeo,Okiyama, Yoshio,Honma, Teruki,Nakata, Akiko,Ito, Akihiro,Yoshida, Minoru,Fujita, Mikako,Otsuka, Masami
, p. 1767 - 1775 (2019)
Bleomycin is considered to exert its antitumor activity via DNA cleavage mediated by activated oxygen generated from the iron complex in its chelator moiety. Spin-offs from this moiety, HPH-1Trt and HPH-2Trt, with anti-cancer activities were recently synt
Investigation of isomer formation upon coordination of bifunctional histidine analogues with 99mTc/Re(CO)3
Simpson, Emily J.,Hickey, Jennifer L.,Breadner, Daniel,Luyt, Leonard G.
, p. 2950 - 2958 (2012/04/10)
Histidine is a convenient tridentate chelator used in the synthesis of technetium-99m radiopharmaceuticals, as it can be pendantly attached to a biomolecule for molecular imaging applications. Once coordinated, it forms a neutral complex that is capable of forming diastereomers at the alpha amine of the histidine. This is demonstrated through the synthesis and characterization of four different histidine chelators; three small molecule chelators, which consist of a benzylated histidine at the alpha amine, and one modified dipeptide, containing a phenylalanine derivative at the C-terminus and a histidine at the N-terminus. Upon rhenium coordination, two products are observed, each having the desired exact mass of the metal-containing species. The two products have been characterized through LC-MS, 1H, gCOSY, NOESY and ROESY NMR experiments, and the relative stereochemistry determined. The implications of diastereomer formation when using this chelation system for creating molecular imaging agents is also discussed.