115148-04-4Relevant articles and documents
Enzyme-artificial enzyme interactions as a means for discriminating among structurally similar isozymes
Selvakumar, Karuthapandi,Motiei, Leila,Margulies, David
, p. 4892 - 4895 (2015)
We describe the design and function of an artificial enzyme-linked receptor (ELR) that can bind different members of the glutathione-S-transferase (GST) enzyme family. The artificial enzyme-enzyme interactions distinctly affect the catalytic activity of the natural enzymes, the biomimetic, or both, enabling the system to discriminate among structurally similar GST isozymes.
Syntheses and anti-HIV and human cluster of differentiation 4 (CD4) down-modulating potencies of pyridine-fused cyclotriazadisulfonamide (CADA) compounds
Lumangtad, Liezel A.,Claeys, Elisa,Hamal, Sunil,Intasiri, Amarawan,Basrai, Courtney,Yen-Pon, Expedite,Beenfeldt, Davison,Vermeire, Kurt,Bell, Thomas W.
, (2020/11/20)
CADA compounds selectively down-modulate human cell-surface CD4 protein and are of interest as HIV entry inhibitors and as drugs for asthma, rheumatoid arthritis, diabetes and some cancers. Postulating that fusing a pyridine ring bearing hydrophobic subst
Coordination chemistry of [Y(pypa)]-and comparison immuno-PET imaging of [44Sc]Sc- And [86Y]Y-pypa-phenyl-TRC105
Li, Lily,de Guadalupe Jaraquemada-Peláez, María,Aluicio-Sarduy, Eduardo,Wang, Xiaozhu,Barnhart, Todd E.,Cai, Weibo,Radchenko, Valery,Schaffer, Paul,Engle, Jonathan W.,Orvig, Chris
, p. 5547 - 5562 (2020/05/13)
Both scandium-44 and yttrium-86 are popular PET isotopes with appropriate half-lives for immuno-positron emission tomography (immuno-PET) imaging. Herein, a new bifunctional H4pypa ligand, H4pypa-phenyl-NCS, is synthesized, conjugate
CHELATORS AND METHODS OF MAKING AND USING SAME
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Paragraph 0087; 0111, (2020/10/09)
A chelating agent having the general formula (I) is provided (I) Metal chelates and constructs for carrying out targeted radionuclide therapy incorporating such chelating agents are provided. Methods of making and using the chelating agent, metal chelates and constructs for carrying out targeted radionuclide therapy, as well as diagnostic and therapeutic methods using such constructs, are provided.
Functionally Versatile and Highly Stable Chelator for 111In and 177Lu: Proof-of-Principle Prostate-Specific Membrane Antigen Targeting
Li, Lily,Jaraquemada-Peláez, María De Guadalupe,Kuo, Hsiou-Ting,Merkens, Helen,Choudhary, Neha,Gitschtaler, Katrin,Jermilova, Una,Colpo, Nadine,Uribe-Munoz, Carlos,Radchenko, Valery,Schaffer, Paul,Lin, Kuo-Shyan,Bénard, Fran?ois,Orvig, Chris
, p. 1539 - 1553 (2019/05/22)
Here, we present the synthesis and characterization of a new potentially nonadentate chelator H4pypa and its bifunctional analogue tBu4pypa-C7-NHS conjugated to prostate-specific membrane antigen (PSMA)-targeting peptidomimetic (Glu-urea-Lys). H4pypa is very functionally versatile and biologically stable. Compared to the conventional chelators (e.g., DOTA, DTPA), H4pypa has outstanding affinities for both 111In (EC, t1/2 ≈ 2.8 days) and 177Lu (β-,?, t1/2 ≈ 6.64 days). Its radiolabeled complexes were achieved at >98% radiochemical yield, RT within 10 min, at a ligand concentration as low as 10-6 M, with excellent stability in human serum over at least 5-7 days (- complexes (M3+ = In3+, Lu3+, La3+) were dependent on the ionic radii, where the smaller In3+ has the highest pM value (30.5), followed by Lu3+ (22.6) and La3+ (19.9). All pM values are remarkably higher than those with DOTA, DTPA, H4octapa, H4octox, and H4neunpa. Moreover, the facile and versatile bifunctionalization enabled by the p-OH group in the central pyridyl bridge of the pypa scaffold (compound 14) allows incorporation of a variety of linkers for bioconjugation through easy nucleophilic substitution. In this work, an alkyl linker was selected to couple H4pypa to a PSMA-targeting pharmacophore, proving that the bioconjugation sacrifices neither the tumor-targeting nor the chelation properties. The biodistribution profiles of 111In- and 177Lu-labeled tracers are different, but promising, with the 177Lu analogue particularly outstanding.
A potent antioxidant small molecule aimed at targeting metal-based oxidative stress in neurodegenerative disorders
Lincoln, Kimberly M.,Gonzalez, Paulina,Richardson, Timothy E.,Julovich, David A.,Saunders, Ryker,Simpkins, James W.,Green, Kayla N.
, p. 2712 - 2714 (2013/05/08)
Metal-ion misregulation and oxidative stress have been linked to the progressive neurological decline associated with multiple neurodegenerative disorders. Transition metal-mediated oxidation of biomolecules via Fenton chemical reactions plays a role in d
Optically active macrocyclic hexaazapyridinophanes decorated at the periphery: Synthesis and applications in the NMR enantiodiscrimination of carboxylic acids
Busto, Eduardo,González-álvarez, Almudena,Gotor-Fernández, Vicente,Alfonso, Ignacio,Gotor, Vicente
experimental part, p. 6070 - 6077 (2010/09/10)
A family of pyridine based dialdehydes has been efficiently prepared starting from chelidamic acid by chemical modification of its 4-hydroxyl group. The condensation of these dialdehydes with commercially available (1R,2R)-(-)-cyclohexane-1,2-diamine in the presence of Ba2+ template led, after the in situ reduction, to the synthesis of a family of enantiopure hexaazapyridinophanes substituted at the periphery. These new receptors have been used as chiral shift agents towards different carboxylic acids. Good splitting of the carboxylic acid NMR signals (up to ΔΔδ=0.13 ppm) were observed using substoichiometrical amount of the receptor.
A new efficient method for the preparation of 2,6-pyridinedimethyl ditosylates from dimethyl 2,6-pyridinedicarboxylates
Horváth, Gy?rgy,Rusa, Cristian,K?nt?s, Zoltán,Gerencsér, János,Huszthy, Péter
, p. 3719 - 3731 (2007/10/03)
We report here an efficient method for the preparation of 2,6- pyridinedimethyl ditosylate and four of its 4-substituted derivatives, two of them have not been reported in the literature. We also describe here a modification of the reported synthesis for chelidonic and chelidamic acids with improved yields and higher purity.
Benzo Condensed Crown Ethers Containing 1,8-Naphthyridine or 4-Pyridone Units - Synthesis and Complex Formation with Organic Guest Molecules
Weber, E.,Koehler, H.-J.
, p. 451 - 455 (2007/10/02)
New crown compounds 3-5 comprising beside o-phenylelene groups 1,8-naphthyridine or 4-pyridone groups as characteristic building units are synthesized.They form numerous stoichiometric crystalline complexes with uncharged organic molecules including alcoh