A5007102751- X-ray Diffraction in Crystallography
- Crystallization and Solubility Studies
- Nanoplatforms for cancer theranostics
- Molecular Sensors and Ion Detection
- Metal complexes synthesis and properties
- Advanced biosensing and bioanalysis techniques
- Quinazolinone synthesis and applications
- N-Heterocyclic Carbenes in Organic and Inorganic Chemistry
- Photoacoustic and Ultrasonic Imaging
- Luminescence and Fluorescent Materials
- Drug Transport and Resistance Mechanisms
- Antibiotic Resistance in Bacteria
- Photodynamic Therapy Research Studies
- Surface Chemistry and Catalysis
- Cystic Fibrosis Research Advances
- Trace Elements in Health
- Lanthanide and Transition Metal Complexes
- Ferrocene Chemistry and Applications
- Cancer Research and Treatments
- Synthesis of Tetrazole Derivatives
- Porphyrin and Phthalocyanine Chemistry
- Metal-Catalyzed Oxygenation Mechanisms
- Synthesis and Characterization of Pyrroles
- Sulfur Compounds in Biology
- Bacterial Genetics and Biotechnology
Ruhr University Bochum
2023-2025
The University of Texas at Austin
2020-2023
An increased demand for iron is a hallmark of cancer cells and thought necessary to promote high cell proliferation, tumor progression metastasis. This makes metabolism an attractive therapeutic target. Unfortunately, current iron-based strategies often lack effectiveness can elicit off-target toxicities. We report here dual-therapeutic prodrug, DOXjade, that allows chelation chemo-photothermal therapy. prodrug takes advantage the clinically approved chelator deferasirox (ExJade®)...
Deferasirox, ExJade, is an FDA-approved iron chelator used for the treatment of overload. In this work, we report several fluorescent deferasirox derivatives that display unique photophysical properties, i.e., aggregation-induced emission (AIE), excited state intramolecular proton transfer, charge and through-bond through-space conjugation characteristics in aqueous media. Functionalization phenol units on scaffold afforded responsive pro-chelator ExPhos, which enabled detection...
New, asymmetric quinizarin-Au(I)-NHC complexes were designed, isolated, and fully characterised including by single crystal X-ray crystallography. Cytotoxicity studies showed effective growth inhibition in HeLa cervical cancer cells with IC
Deferasirox, an FDA-approved iron chelator, has gained increasing attention for use in anticancer and antimicrobial applications. Recent efforts by our group led to the identification of this core as easy-to-visualize aggregation-induced emission platform, or AIEgen, that provides a therapeutic effect equivalent deferasirox (J. Am. Chem. Soc. 2021, 143, 3, 1278–1283). However, wavelength first-generation system overlapped with Syto9, green emissive dye used indicate live cells. Here, we...
Over the past 30 years fluorescent chemosensors have evolved to incorporate many optical-based modalities and strategies. In this perspective we seek highlight current state of art as well provide our viewpoint on most significant future challenges remaining in area. To underscore trends field facilitate understanding area, reader with appropriate contemporary examples. We then conclude thoughts probable directions that chemosensor development will take not-too-distant future.
Metal chelators belonging to the di-pyridyl-thiosemicarbazone (DpTs) class have shown great promise as adjuvant therapeutics for treating cancer, with DpC and Dp44mT emerging lead candidates. Despite their potency, these molecules also induce various undesirable side effects due insufficient cancer cell targeting, highlighting need improve selectivity. Here, we present a first generation of DpT-antibody conjugates. To this end, developed facile synthesis functionalize DpTs strategically...
We report here strategic functionalization of the FDA approved chelator deferasirox (1) in an effort to produce organelle-targeting iron chelators with enhanced activity against A549 lung cancer cells.
Deferasirox is an FDA-approved iron chelator used in the treatment of toxicity. In this work, we report use several deferasirox derivatives as lanthanide chelators. Solid-state structural studies three representative trivalent cations, La(III), Eu(III), and Lu(III), revealed formation 2:2 complexes solid state. A 1:1 stoichiometry dominates DMSO solution, with Ka values 472 ± 14, 477 11, 496 15 M-1 being obtained case these respectively. Under conditions competitive precipitation presence...
Deferasirox, ExJade , an FDA-approved treatment for iron overload disorders has been shown to inhibit the growth of both gram-positive and -negative bacteria through (Fe(III)) chelation. Modification framework led identification a new fluorescent platform ExPh ExBT . Functionalization phenol moieties on with phosphate units afforded ratiometric pro-chelator ( ExPhos ), which was effective in inhibition two clinically relevant antibiotic-resistant bacteria, (MRSA (ATCC 43300) VRE 51299)),...
<p>Deferasirox,<b> ExJade</b>, an FDA-approved treatment for iron overload disorders has been shown to inhibit the growth of both gram-positive and -negative bacteria through (Fe(III)) chelation. Modification <b>ExJade</b> framework led identification a new fluorescent platform <b>ExPh </b>and <b>ExBT</b>. Functionalization phenol moieties on <b>ExBT</b> with phosphate units afforded ratiometric pro-chelator...
Herein, we describe a detailed preparation of the versatile pyrrole building block 3,4-diethylpyrrole-2-carboxylate (1), key structural feature in various porphyrins, porphyrinoids, and other chromophores. 1 was prepared via one-pot DBU catalyzed Henry reaction acid acetylation followed by an aqueous workup telescoping through adapted Magnus-Schöllkopf-Barton-Zard cyclization protocol from commercial starting materials. The three-step utilized new chemistry, requires only one formal...
Here, we report that ExSO3H, a synthetically accessible, water-soluble, non-toxic derivative of the clinical iron chelator deferasirox, acts as colorimetric chemosensor permits detection and quantification Fe3+ in aqueous samples at pH 2–5. In addition, observed fluorescent turn-on response was produced when this allowed to interact with human serum albumin (HSA). This fluorescence quenched presence Fe3+, thus allowing us monitor biologically important metal cation via two independent methods.