A5006222361- Radiopharmaceutical Chemistry and Applications
- Synthesis and Catalytic Reactions
- Medical Imaging Techniques and Applications
- Chemical Synthesis and Analysis
- X-ray Diffraction in Crystallography
- Crystallization and Solubility Studies
- Molecular Sensors and Ion Detection
- Supramolecular Chemistry and Complexes
- Monoclonal and Polyclonal Antibodies Research
- Lanthanide and Transition Metal Complexes
- Medical Imaging and Pathology Studies
- Asymmetric Synthesis and Catalysis
- Catalytic C–H Functionalization Methods
- Crystallography and molecular interactions
- Synthesis and Biological Evaluation
- Synthesis of β-Lactam Compounds
- Metal complexes synthesis and properties
- Lung Cancer Treatments and Mutations
- Mass Spectrometry Techniques and Applications
- Hemoglobinopathies and Related Disorders
- Oxidative Organic Chemistry Reactions
- Peptidase Inhibition and Analysis
- Axial and Atropisomeric Chirality Synthesis
- HER2/EGFR in Cancer Research
- Asymmetric Hydrogenation and Catalysis
Illinois Institute of Technology
2012-2025
Montefiore Medical Center
2015
National Cancer Institute
2001-2008
National Institutes of Health
2002-2008
Center for Cancer Research
2006-2008
Physical Sciences (United States)
2007-2008
Wake Forest University
2002-2004
University of North Texas
1996-2002
Texas Christian University
2001
We report a practical and high-yield synthesis of bimodal bifunctional ligand 3p-C-NETA-NCS containing the isothiocyanate group for conjugation to tumor targeting antibody. was conjugated tumor-targeting antibody, trastuzumab, corresponding 3p-C-NETA-trastuzumab conjugate evaluated compared trastuzumab conjugates known ligands C-DOTA, C-DTPA, 3p-C-DEPA radiolabeling kinetics with 90Y 177Lu. exhibited extremely rapid complexation 90Y-3p-C-NETA-trastuzumab 177Lu-3p-C-NETA-trastuzumab were...
Novel 1,4,7-triazacyclononane-N,N',N' '-triacetic acid (NOTA) based octadentate ligands [2-(4,7-biscarboxymethyl[1,4,7]triazacyclononan-1-ylethyl)carbonylmethylamino]acetic tetrahydrochloride (1) and [3-(4,7-biscarboxymethyl[1,4,7]triazacyclononan-1-yl-propyl)carbonylmethylamino]acetic (2) with pendent donor groups as potential yttrium chelators for radioimmunotherapy (RIT) have been prepared via a convenient high-yield cyclization route. The complexation kinetics of the novel chelates...
A new bifunctional ligand 3p-C-DEPA was synthesized and evaluated for use in targeted α-radioimmunotherapy. efficiently prepared via regiospecific ring opening of an aziridinium ion conjugated with trastuzumab. The 3p-C-DEPA-trastuzumab conjugate extremely rapid binding (205/6)Bi, the corresponding (205/6)Bi-3p-C-DEPA-trastuzumab complex stable human serum. Biodistribution studies were performed to evaluate vivo stability tumor targeting bearing athymic mice. displayed excellent as evidenced...
Electrospray ionization (ESI)/quadrupole ion trap mass spectrometry is used to evaluate the heavy metal binding selectivities of five caged crown ethers and two polyether reference compounds in methanol solution. The preferences for Hg2+, Pb2+, Cd2+, Cu2+ were analyzed by comparison ESI spectral intensities with aim developing this method rapid screening new synthetic ligands. cage preferentially bind except cryptand derivative, which favors Pb2+. preference Hg2+ stems from favorable...
The structurally novel bifunctional ligands C-NETA and C-NE3TA, each possessing both acyclic macrocyclic moieties, were prepared evaluated as potential chelates for radioimmunotherapy (RIT) targeted magnetic resonance imaging (MRI). Heptadentate C-NE3TA was fortuitously discovered during the preparation of C-NETA. An optimized synthetic method to including purification polar tailing reaction intermediates, tert-butyl (2) (3) using semiprep HPLC developed. new Gd(III) complexes contrast...
A novel bifunctional ligand (3p-C-NETA) for antibody-targeted radioimmunotherapy of 90Y and 177Lu was efficiently synthesized <italic>via</italic> regiospecific ring opening an aziridinium ion.
The great promise of iron depletion as a therapeutic strategy for various diseases, including overload, cancers, Alzheimer's disease, Parkinson's tuberculosis, HIV, and fungal malaria infection, has stimulated research on the development chelators agents. In November 2005, FDA approved deferasirox (ICL670A; Exjade®), first once-daily oral drug treatment chronic overload. So far, five chelators, deferoxamine, deferiprone, deferasirox, dexrazorane ciclopirox, have been use in anticancer or...
An antibody-targeted radiation therapy (radioimmunotherapy, RIT) employs a bifunctional ligand that can effectively hold cytotoxic metal with clinically acceptable complexation kinetics and stability while being attached to tumor-specific antibody. Clinical exploration of the therapeutic potential RIT has been challenged by absence adequate ligand, critical component for enhancing efficacy cancer therapy. To address this deficiency, C-NETA in unique structural class possessing both...
Novel chelates PIP−DTPA, AZEP−DTPA, NETA, NPTA, and PIP−DOTA were synthesized evaluated as potential magnetic resonance imaging (MRI) contrast enhancement agents. The T1 T2 relaxivities of their corresponding Gd(III) complexes are reported. At clinically relevant field strengths, the comparable to that used agents Gd(DTPA) Gd(DOTA). serum stability 153Gd-labeled complexes, Gd(PIP−DTPA), Gd(AZEP−DTPA), Gd(PIP−DOTA), Gd(NETA), Gd(NPTA), was assessed by measuring release 153Gd from complexes....
Bile acid–polyaminocarboxylate conjugates containing NE3TA, a potential iron chelator displayed significant cytotoxicities in both HeLa and HT29 colon cancer cells, cholic acid–NE3TA attached to an organic fluorophore was shown enter the cells.
Microelectrospray ionization mass spectrometry (MESI-MS) is used to evaluate alkali metal binding selectivities of a variety macrocyclic compounds. Well-studied crown ethers are validate the MESI-MS method. A quantitative correlation between MESI spectral ion intensities and solution equilibrium distributions complexes obtained for mixtures containing single host different guest ions. The method successfully applied determination series cage-functionalized aza-crown relevant model compounds...
Two DTPA derivatives (PIP-DTPA and AZEP-DTPA) as potential contrast enhancement agents in MRI are synthesized. The T1 T2 relaxivities of their corresponding Gd(III) complexes reported. At clinically relevant field strengths, the comparable to that agent, Gd(DTPA) which is clinical use. serum stability (153)Gd-labeled assessed by measuring release (153)Gd from ligands. radiolabeled Gd chelates found be kinetically stable human for up at least 14 days without any measurable loss radioactivity.
Iron depletion, using iron chelators targeting transferrin receptor (TfR) and ribonucleotide reductase (RR), is proven to be effective in the treatment of cancer. We synthesized evaluated novel polyaminocarboxylate-based NETA, NE3TA, NE3TA-Bn their bifunctional versions C-NETA, C-NE3TA, N-NE3TA for use depletion tumor therapy. The cytotoxic activities polyaminocarboxylates were HeLa HT29 colon cancer cell lines compared clinically available agent DFO frequently explored polyaminocarboxylate...
Various aziridinium salts were efficiently prepared from bromination of a series backbone substituted N,N-bisubstituted β-amino alcohols and isolated via flash column chromatography. The effect C-substitution, N-substitution, solvent, leaving group, counteranions on formation the isolable was investigated.