342635-34-1Relevant articles and documents
Linkage effects on binding affinity and activation of GPR30 and estrogen receptors ERα/β with tridentate pyridin-2-yl hydrazine tricarbonyl-Re/99mTc(I) chelates
Ramesh, Chinnasamy,Bryant, Bj,Nayak, Tapan,Revankar, Chetana M.,Anderson, Tamara,Carlson, Kathryn E.,Katzenellenbogen, John A.,Sklar, Larry A.,Norenberg, Jeffrey P.,Prossnitz, Eric R.,Arterburn, Jeffrey B.
, p. 14476 - 14477 (2006)
We describe a new structural class of neutral tridentate pyridin-2-yl hydrazine chelates for labeling with tricarbonyl Re/99mTc(I) under aqueous conditions and investigate the receptor binding of synthetic estradiol derivatives with the novel G-protein-coupled receptor GPR30 and estrogen receptors ERα/β. The steroid linkage affected the affinity and selectivity of estrogen binding with these receptors. Fluorescence assays based on calcium signaling demonstrate that membrane-permeable chelates 2 and 3 interact with the receptors in whole cells. These results suggest that in vitro assays will facilitate the development of targeted imaging agents for intracellular receptors and the feasibility of targeting GPR30 and ERα/β for diagnostic tumor imaging. Copyright
Synthesis of 17-α-substituted estradiol-pyridin-2-yl hydrazine conjugates as effective ligands for labeling with Alberto's complex fac-[Re(OH2)3(CO)3]+ in water
Arterburn, Jeffrey B.,Corona, Cesear,Rao, Kalla Venkateswara,Carlson, Kathryn E.,Katzenellenbogen, John A.
, p. 7063 - 7070 (2003)
The development of 99mTc-estradiol radiopharmaceuticals would be advantageous for the detection of estrogen receptor-positive breast tumors. Estradiol derivatives conjugated to organometallic tricarbonyl-Tc(I) and related Re(I) complexes are ca
Catalytic amination of 2-substituted pyridines with hydrazine derivatives.
Arterburn,Rao,Ramdas,Dible
, p. 1351 - 1354 (2007/10/03)
[reaction in text] Protected pyridylhydrazine derivatives were prepared in a one-step palladium-catalyzed amination reaction using chelating phosphine ligands. 2-Pyridyl chlorides, bromides, and triflates were effective electrophiles in these reactions. Di-tert-butyl hydrazodiformate was an excellent hydrazine substrate, and the resulting products were deprotected under mild conditions. Catalytic amination provides a direct route to protected bifunctional hydrazinopyridine linkers that are suitable for metal-bioconjugate syntheses.