A5076232137- Ferrocene Chemistry and Applications
- Metal complexes synthesis and properties
- Synthesis and Biological Evaluation
- Crystallization and Solubility Studies
- Peptidase Inhibition and Analysis
- Drug Transport and Resistance Mechanisms
- X-ray Diffraction in Crystallography
- Lung Cancer Diagnosis and Treatment
- Ferroptosis and cancer prognosis
- Radiomics and Machine Learning in Medical Imaging
- Synthesis and biological activity
- Crystallography and molecular interactions
- Click Chemistry and Applications
- Hip disorders and treatments
- RNA Interference and Gene Delivery
- Medical Imaging and Pathology Studies
- Plant-based Medicinal Research
- Catalytic Cross-Coupling Reactions
- Synthesis and Reactivity of Heterocycles
- MicroRNA in disease regulation
- Catalytic C–H Functionalization Methods
- Glycosylation and Glycoproteins Research
- Dendrimers and Hyperbranched Polymers
- Hip and Femur Fractures
- Synthesis of Organic Compounds
Qingdao National Laboratory for Marine Science and Technology
2022-2025
Ocean University of China
2022-2025
Chimie ParisTech
2015-2024
Sorbonne Université
2015-2024
Chinese Academy of Sciences
2011-2024
University College Dublin
2024
Marine Biomedical Research Institute of Qingdao
2024
Beijing University of Chinese Medicine
2024
Fudan University
2024
Shanghai Institute of Organic Chemistry
2024
A [2+2+2] modular synthesis of multisubstituted pyridines, with excellent regioselectivity, has been realized by copper catalysisand involves three distinct components: vinyliodonium salts, nitriles, and alkynes. The reactions proceeded the facile formation an aza-butadienylium intermediate alkenylation nitrile a salt. Moreover, alkynes in reaction were extended to alkenes, which are advantage expense relative scarceness
Ferroptosis has emerged as a form of programmed cell death and exhibits remarkable promise for anticancer therapy. However, it is challenging to discover ferroptosis inducers with new chemotypes high ferroptosis-inducing potency. Herein, we report series ferrocenyl-appended GPX4 inhibitors rationally designed in "one stone kills two birds" strategy. selectivity assays, inhibitory activity CETSA experiments validated the inhibition novel compounds on GPX4. In particular, ROS-related...
Redox‐based diagnostic and therapeutic applications have long suffered from a shortage of suitable drugs probes high specificity. In the context anti‐ferroptosis research for neurological diseases, inaccessibility blood‐brain barrier permeable (BBB) small molecular ferroptosis inhibitor, lack specific seriously impeded deeper understanding mechanism development clinically applicable drugs. We here report novel 1,3,4‑thiadiazole‐functionalized drug‐like ferrostatin analogue entitled...
Abstract The synthesis and chemical oxidation profile of a new generation ferrocifen derivatives with strong antiproliferative behavior in vitro is reported. In particular, the hydroxypropyl derivative HO(CH 2 ) 3 C(Fc)=C(C 6 H 4 OH) ( b exhibited exceptional activity against cancer cell lines HepG2 MDA‐MB‐231 TNBC, IC 50 values 0.07 0.11 μ M , respectively. Chemical yielded an unprecedented tetrahydrofuran‐substituted quinone methide (QM) via internal cyclization hydroxyalkyl chain, whereas...
In this study, cationic nanoparticles self-assembled from the amphiphilic copolymer poly(N-methyldietheneamine sebacate)-co-[(cholesteryl oxocarbonylamido ethyl) methyl bis(ethylene) ammonium bromide] sebacate) (P(MDS-co-CES) were synthesized and used to deliver Bcl-2 targeted siRNA into HepG2, HeLa MDA-MB-231 cell lines, downregulate mRNA expression levels. Confocal microscopic studies show that able complex with it inside cells efficiently, but was easily dissociated complexes in cytoplasm...
The success of targeted covalent inhibitors (TCIs) for treating cancers has spurred the search novel scaffolds to install warheads. In our endeavour, using a scaffold hopping strategy, we managed utilize imidazo[1,2-
Among a large number of HIV-1 integrase (IN) inhibitors, the 8-hydroxy-[1,6]naphthyridines (i.e., L-870,810) were one promising class antiretroviral drugs developed by Merck Laboratories. In spite its remarkable potency and efficacy, unfortunately upon completion phase I clinical studies, development L-870,810 was halted. Because desirable pharmacological pharmaceutical properties we intrigued to design novel analogues with goals (1) improve limitations naphthyridine-7-carboxamides as...
Ferrociphenols are known to display anticancer properties by original mechanisms dependent on redox and generation of active metabolites such as quinone methides. Recent studies have highlighted the positive impact oxidative stress chemosensitivity prognosis ovarian cancer patients. Ovarian adenocarcinomas shown be an excellent model for defining selected ferrociphenols new therapeutic drugs cancers. This work describes syntheses preliminary mechanistic research unprecedented multitargeting...
Organometallic compounds bearing the redox motif [ferrocenyl-
Oxidized low-density lipoprotein (oxLDL) indu-ces macrophage inflammation and lipid uptake, serves important roles in the development of atherosclerosis. The long non-coding RNA (lncRNA) nuclear paraspeckle assembly transcript 1 (neat1) has two isoforms; longer isoform, neat1_2, mediates formation subnuclear structures called paraspeckles. Reverse transcription‑quantitative polymerase chain reaction (RT‑qPCR), western blotting protein immunoprecipitation (RIP), revealed that oxLDL induced...
Ferrociphenols, especially those possessing a heterocycle at the terminus of an aliphatic chain, display strong anticancer activity through novel redox mechanism that generates active metabolites such as quinone methides (QMs). X-ray crystallography and UV/Vis spectroscopy reveal specific lone pair (lp)-π interaction between carbonyl group imide motif QM plays important role in exceptional cytotoxic behaviour their imido-ferrociphenol precursors. This intramolecular lp-π markedly enhanced...
Novel ROS-responsive N -alkylaminoferrocene (NAAF)-appended GPX4 inhibitors have been designed and prepared as potent ferroptosis-inducing prodrugs.
Redox‐based diagnostic and therapeutic applications have long suffered from a shortage of suitable drugs probes high specificity. In the context anti‐ferroptosis research for neurological diseases, inaccessibility blood‐brain barrier permeable (BBB) small molecular ferroptosis inhibitor, lack specific seriously impeded deeper understanding mechanism development clinically applicable drugs. We here report novel 1,3,4‑thiadiazole‐functionalized drug‐like ferrostatin analogue entitled...
Abstract Ferrociphenols ( FCs ) and their oxidized, electrophilic quinone methide metabolites FC‐QMs are organometallic compounds related to tamoxifen that exhibit strong antiproliferative properties. To evaluate the reactivity of toward cellular nucleophiles, we studied reaction with selected thiols. A series new resulting from addition these FC‐SR adducts, were thus synthesized completely characterized. Such conjugates formed upon metabolism by liver microsomes in presence NADPH Some...
Ferrocidiphenols possessing appropriate substituents in the aliphatic chain have very promising anticancer properties, but a systematic approach to deciphering their diversified metabolic behavior has so far been lacking. Herein, we show that series of novel ferrocidiphenols bearing different hydroxyalkyl exhibit strong activity as revealed range vitro and vivo experiments. Moreover, they display oxidative transformation profiles distinct from those previous complexes, shown by use chemical...
Cyrhetrenyl [η<sup>5</sup>-C<sub>5</sub>H<sub>4</sub>Re(CO)<sub>3</sub>] tag allows localization of a cytotoxic iron/rhenium dimetallic complex in the nucleus single MDA-MB-231 breast cancer cell.
An efficient and easy procedure to synthesize the pyridinyl analogues of dibenzylideneacetone (pyr-dba) was developed by condensation substituted nicotinaldehyde acetone in presence K(2)CO(3) toluene-EtOH-H(2)O solvent system. Structurally diverse pyr-dba, including quinolinyl dba, can be prepared conveniently moderate excellent yields under mild conditions with this method. The resulting pyr-dba functioned as enone analogs curcumin efficiently inhibited activation NF-κB growth colorectal...