A5074575233- Synthesis and biological activity
- Pharmacological Effects of Natural Compounds
- Bioactive Compounds and Antitumor Agents
- Research on Leishmaniasis Studies
- Dermatology and Skin Diseases
- Catalytic Cross-Coupling Reactions
- Herbal Medicine Research Studies
- Genomics and Chromatin Dynamics
- Plant-derived Lignans Synthesis and Bioactivity
- Cytokine Signaling Pathways and Interactions
- Traditional and Medicinal Uses of Annonaceae
- Fungal Plant Pathogen Control
- Multiple Sclerosis Research Studies
- Phytochemistry and Bioactivity Studies
- Genetic Associations and Epidemiology
- Computational Drug Discovery Methods
- Phytochemistry and biological activity of medicinal plants
- Pharmacological Receptor Mechanisms and Effects
- Psoriasis: Treatment and Pathogenesis
- BRCA gene mutations in cancer
- Allergic Rhinitis and Sensitization
- Advanced Synthetic Organic Chemistry
- Morinda citrifolia extract uses
- Coordination Chemistry and Organometallics
- Nicotinic Acetylcholine Receptors Study
Leo Pharma (Denmark)
2019-2021
Copenhagen University Hospital
2005-2015
Herlev Hospital
2014-2015
Population Council
2015
Leo Pharma (Australia)
2005-2014
Cancer Research UK
2014
University of Copenhagen
2014
Gentofte Hospital
2014
Technical University of Denmark
2005
Schools of Visual Arts, The Royal Danish Academy of Fine Arts
1997-2000
A large number of substituted chalcones have been synthesized and tested for antileishmanial lymphocyte-suppressing activities. subset the was designed by using statistical methods. 3D-QSAR analyses 67 (antileishmanial activity) 63 (lymphocyte-suppressing compounds training sets 9 as an external validation set were performed GRID/GOLPE methodology. The Smart Region Definition procedure with subsequent region selection implemented in GOLPE reduced variables to approximately 1300 yielding...
In the past few years focus on central acetylcholine receptors has shifted from compounds with affinity for muscarinic (mAChR) to nicotinic (nAChR). The therapeutic potential includes treatment of a variety diseases, e.g., Alzheimer's disease, Parkinson's and Tourette's syndrome. This work describes synthesis six novel series potent ligands nanomolar α4β2 nAChR subtype. Structure−activity relationship (SAR) was evaluated by calculation 3D-QSAR model. analysis using GRID/GOLPE methodology...
This paper describes how the introduction of "cationic" aliphatic amino groups in chalcone scaffold results potent antibacterial compounds. It is shown that most favorable position for group 2-position B-ring, particular combination with a lipophilic substituent 5-position B-ring. We demonstrate compounds act by unselective disruption cell membranes. Introduction an additional A-ring are selective bacterial membranes combined high activity against both Gram-positive and -negative pathogens....
Abstract The coupling reaction of diverse arylhalogenids with phenyl-boronic acid under solvent-free conditions has been performed using a palladium catalyst. order reactivity was complementary to the normal Suzuki reaction.
We recently identified a novel susceptibility variant, rs865686, for estrogen-receptor positive breast cancer at 9q31.2. Here, we report fine-mapping analysis of the 9q31.2 locus using 43 160 cases and 42 600 controls European ancestry ascertained from 52 studies further 5795 6624 Asian nine studies. Single nucleotide polymorphism (SNP) rs676256 was most strongly associated with risk in Europeans (odds ratios [OR] = 0.90 [0.88–0.92]; P-value 1.58 × 10−25). This SNP is one cluster highly...
Recent genome-wide association studies (GWAS) and subsequent meta-analyses have identified over 25 SNPs at 18 loci, together accounting for >15% of the genetic susceptibility to testicular germ cell tumour (TGCT). To identify further common associated with TGCT, here we report a three-stage experiment, involving 4098 cases 972 controls. Stage 1 comprised previously published GWAS analysis 307 291 in 986 4946 In 2, used customised Illumina iSelect genotyping array (iCOGs) data across 694 1064...
The absolute configuration of the norlignan (+)-nyasol was determined to be S by comparison experimental vibrational circular dichroism data with first-principle calculations taking into account eight lowest energy conformations. established enables establishment (−)-hinokiresinol, which is concluded S. A total synthesis and resolution hinokiresinol has been performed resolve conflicting reports coupling constant vinylic protons disubstituted double bond in this molecule. Racemic resolved....
We describe the design of a novel PDE4 scaffold and exploration dual-soft concept to reduce systemic side effects via rapid elimination: introducing ester functionalities that can be inactivated in blood as well by liver (dual-soft) while being stable human skin. Compound 40 was selected clinical candidate it potent rapidly degraded inactive metabolites because preclinical studies showed high exposure at target organ: Preclinical data are presented confirming value reducing exposure.
The known KDR inhibitor SU5416 and several analogues of the indolin-2-one family were surprisingly found to be highly efficacious in EAE model, an established model for multiple sclerosis. high vivo effect could correlated vitro inhibition pro-inflammatory cytokine IL-2. Activity following po administration was obtained with via use prodrugs.
A systematic change of the substituents and side chain norneolignan hinokiresinol afforded a 10 fold improvement IC50 value toward inhibition growth Plasmodium falciparum. The more potent compounds controlled parasitemia in mice infected with berghei.
Interleukin 17 (IL-17) cytokines promote inflammatory pathophysiology in many autoimmune diseases, including psoriasis, multiple sclerosis, rheumatoid arthritis, and bowel disease. Such broad involvement of IL-17 various diseases makes it an ideal target for drug discovery. Psoriasis is a chronic disease characterized by numerous defective components the immune system. Significantly higher levels IL-17A have been noticed lesions psoriatic patients, if compared to non-lesion parts. Therefore,...
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Abstract ChemInform is a weekly Abstracting Service, delivering concise information at glance that was extracted from about 100 leading journals. To access of an article which published elsewhere, please select “Full Text” option. The original trackable via the “References”
Abstract ChemInform is a weekly Abstracting Service, delivering concise information at glance that was extracted from about 100 leading journals. To access of an article which published elsewhere, please select “Full Text” option. The original trackable via the “References”