A5072354686- Cancer, Hypoxia, and Metabolism
- Photochromic and Fluorescence Chemistry
- Click Chemistry and Applications
- Estrogen and related hormone effects
- Synthesis and biological activity
- Synthesis of Organic Compounds
- Cancer Treatment and Pharmacology
- Luminescence and Fluorescent Materials
- Plant-derived Lignans Synthesis and Bioactivity
- Computational Drug Discovery Methods
- Alzheimer's disease research and treatments
- Melanoma and MAPK Pathways
- Molecular Sensors and Ion Detection
- Pituitary Gland Disorders and Treatments
- Phytochemistry and Biological Activities
- Lanthanide and Transition Metal Complexes
- X-ray Diffraction in Crystallography
- Cholinesterase and Neurodegenerative Diseases
- Synthesis and Characterization of Heterocyclic Compounds
- Growth Hormone and Insulin-like Growth Factors
- Crystallization and Solubility Studies
- Catalytic C–H Functionalization Methods
- Phytochemistry and Bioactive Compounds
- Lipid metabolism and biosynthesis
- Synthesis of Indole Derivatives
Uppsala University
2020-2024
Linköping University
2015-2017
Simon Fraser University
2014-2017
Burnaby Hospital
2017
University of Gothenburg
2009-2016
Ludwig Cancer Research
2013
Uppsala University Hospital
2013
Metabolic reprogramming is critical during clear cell renal carcinoma (ccRCC) tumorigenesis, manifested by accumulation of lipid droplets (LDs), organelles that have emerged as new hallmarks cancer. Yet, regulation their biogenesis still poorly understood. Here, we demonstrate MYC inhibition in ccRCC cells lacking the von Hippel Lindau ( VHL ) gene leads to increased triglyceride content potentiating LD formation a glutamine-dependent manner. Importantly, concurrent signaling and glutamine...
A series of multi-target-directed ligands are described that bind Cu, act as antioxidants, modulate Aβ peptide aggregation, and abolish toxicity in primary neurons.
Altered lipid metabolism and extensive storage in cells have been associated with various medical disorders, including cancer. The development of fluorescent probes that specifically accumulate deposits is therefore great interest order to study pathological processes are linked dysregulated lipogenesis. In the present study, we a small benzothiadiazole dye stains droplets living fixated cells. photophysical characterization probe revealed strong solvatochromic behavior, large Stokes shifts,...
A base-promoted condensation between 2-hydroxyacetophenones and aliphatic aldehydes has been studied. The reaction optimized to afford 2-alkyl-substituted 4-chromanones in an efficient manner using microwave heating. Performing the diisopropylamine EtOH at 170 degrees C for 1 h gave moderate high yields (43-88%). could be further converted into highly functionalized 2,3,6,8-tetrasubstituted chromones which a 3-substituent (acetate, amine, or bromine) was introduced via straightforward...
Abstract A series of 8‐(1 H ‐1,2,3‐triazol‐4‐yl)‐substituted adenosine derivatives have been synthesised by using Sonogashira cross‐coupling and click chemistry. The use chemistry enables an easy access to different substituents in the 4‐position triazole ring. modified nucleosides show high absorptivities due a single strongly allowed electronic transition and, for some derivatives, quantum yields organic as well water solution making them promising fluorescent probes nucleic acid contexts....
3-(4-Fluorophenyl)-2-(4-pyridyl)chromone derivatives were synthesized and evaluated as p38 MAP kinase inhibitors. Introduction of an amino group in the 2-position pyridyl moiety gave p38α inhibitors with IC(50) low nanomolar range (e.g., = 17 nm). The showed excellent selectivity profiles when tested on a panel 62 kinases, well efficient inhibition signaling human breast cancer cells.
Fluorescent scaffolds that can be easily modified<italic>via</italic>click chemistry were investigated as probes for Aβ-plaque deposits in mouse tissue.
Shake, Rattle and Gold! Mechanochemistry enables the efficient selective synthesis of organo-Au(<sc>i</sc>) complexes.
Abstract This minireview describes the syntheses, structure‐photophysical properties relationship, and bioimaging applications of fluorescent coumarins, xanthenes, BODIPYs, cyanines. Advantages disadvantages emissive units are also discussed, as general practical issues that need to be considered when using fluorophores in a biological setting.
Background The AKT/mTORC1/S6K pathway is frequently overstimulated in breast cancer, constituting a promising therapeutic target. benefit from mTOR inhibitors varies, likely as consequence of tumour heterogeneity, and upregulation several compensatory feed-back mechanisms. mTORC1 downstream effectors S6K1, S6K2, 4EBP1 are amplified overexpressed associated with poor outcome divergent endocrine treatment benefit. S6K1 S6K2 share high sequence homology, but evidence partly distinct biological...
Abstract In this study, we present a series of solvatochromic phenylbenzothiadiazoles that display dual emission from the locally excited (LE) and intramolecular charge transfer (ICT) states. The donor‐acceptor derivatives are highly sensitive to polarity changes, which can be monitored by differences in efficiency, spectroscopic shifts variations LE/ICT ratio. One compounds series, containing thiomethyl substituent, emerged as an excellent blue emitting stain for intracellular lipid...
Abstract We present the synthesis and photophysical characterisation of a series structurally diverse, fluorescent 2,6,8‐trisubstituted 3‐hydroxychromone derivatives with high fluorescence quantum yields molar extinction coefficients. Two these ( 9 10 ) have been studied as fluorophores for cellular imaging in HeLa cells show excellent permeability promising properties environment. In addition, we demonstrated by 3‐isobutyroxychromone that esterification 3‐hydroxyl group results acceptable...
In this work, a series of fluorescent 2,1,3-benzothiadiazole derivatives with various N-substituents in the 4-position was synthesized and photophysically characterized solvents. Three compounds emerged as excellent probes for imaging lipid droplets cancer cells. A correlation between their high lipophilicity droplet specificity could be found, log P ≥ 4 being characteristic accumulation.
A series of 2,1,3-benzothiadiazole–Au( i )–L complexes have been synthesised, structurally characterised and investigated for their photophysical properties.
The 2,1,3-benzothiadiazole (BTD) unit is a prominent building block commonly used in various research areas such as optoelectronics and bioimaging. Despite its great versatility, the development of strategies to elaborate BTD has been largely neglected, including exploring reactivity understanding how regioselective functionalization can be tune fluorescence emission. Previous focus primarily on C4- or C4,C7-substitutions. Here, series unsymmetrical mono - disubstituted BTDs was synthesized...
Abstract The insulin-like growth factor-1 (IGF-I) and its receptors play an important role in transformation progression of several malignancies. Inhibitors this pathway have been developed evaluated but generally performed poorly clinical trials, drug candidates abandoned. cyclolignan picropodophyllin (PPP) has described as a potent selective IGF-IR inhibitor is currently undergoing trials. We investigated PPP's activity panels human cancer cell lines (e.g., esophageal squamous carcinoma...
We present an extensive photophysical study of a series fluorescent indolylbenzothiadiazole derivatives and their ability to specifically image lipid droplets in astrocytes glioblastoma cells. All compounds the displayed positive solvatochromism together with large Stokes shifts, π-extended exhibited elevated brightness. It was shown that fluorescence properties were highly tunable by varying electronic character or size N-substituent on indole motif. Three proved capable as probes for...
The study of a fluorescent indolin-3-one derivative is reported that, as opposed to its previously described congeners, selectively undergoes photoactivated ring-opening in apolar solvents. excited state involved this photoisomerization was partially deactivated by the formation singlet oxygen. Cell studies revealed lipid droplet accumulation and efficient light-induced cytotoxicity.
Despite growing interest in 2,1,3-benzothiadiazole (BTD) as an integral component of many functional molecules, methods for the functionalization its benzenoid ring have remained limited, and even simply decorated BTDs required de novo synthesis. We show that regioselective Ir-catalyzed C–H borylation allows access to versatile 5-boryl or 4,6-diboryl BTD building blocks, which undergo at C4, C5, C6, C7 positions. The optimization regioselectivity are discussed. A broad reaction scope is...