A5040514475- Alkaloids: synthesis and pharmacology
- Chemical Synthesis and Analysis
- Advanced Breast Cancer Therapies
- Chemical synthesis and alkaloids
- Prostate Cancer Treatment and Research
- Protein Degradation and Inhibitors
- Synthesis and Reactivity of Heterocycles
- Oxidative Organic Chemistry Reactions
- Lung Cancer Treatments and Mutations
- Chemical Synthesis and Reactions
- HER2/EGFR in Cancer Research
- Click Chemistry and Applications
- Multicomponent Synthesis of Heterocycles
- Radical Photochemical Reactions
- Cyclopropane Reaction Mechanisms
- Asymmetric Synthesis and Catalysis
- Microbial Natural Products and Biosynthesis
- Retinoids in leukemia and cellular processes
- Synthesis and Biological Activity
- Advanced Synthetic Organic Chemistry
- Vanadium and Halogenation Chemistry
- Nuclear Receptors and Signaling
- Synthetic Organic Chemistry Methods
- Microtubule and mitosis dynamics
- Cancer, Hypoxia, and Metabolism
University of Ioannina
2011-2025
Arqule (United States)
1998-2012
National Centre of Scientific Research "Demokritos"
2010
Brown University
1993-2005
A highly efficient and versatile method for the synthesis of benzimidazoles was achieved in one step via Na2S2O4 reduction o-nitroanilines presence aldehydes. Heating a solution o-nitroaniline (1c) an aldehyde EtOH or another appropriate solvent, aqueous solid Na2S2O4, provided facile access to series 2-substituted N-H 5a-m containing wide range functional groups not always compatible with existing synthetic methods. This methodology has also been applied regioselective N-alkyl N-aryl 6a-f...
Parkinson's disease (PD) is a progressive neurodegenerative disorder characterized by the loss of dopaminergic (DAergic) neurons in substantia nigra and gradual depletion dopamine (DA). Current treatments replenish DA deficit improve symptoms but induce dyskinesias over time, neuroprotective therapies are nonexistent. Here we report that Nuclear receptor-related 1 (Nurr1):Retinoid X receptor α (RXRα) activation has double therapeutic potential for PD, offering both symptomatic improvement....
ADVERTISEMENT RETURN TO ISSUEPREVArticleNEXTConvergent synthesis of (.+-.)-dihydroisocodeine in 11 steps by the tandem radical cyclization strategy. A formal total (.+-.)-morphineKathlyn A. Parker and Demosthenes FokasCite this: J. Am. Chem. Soc. 1992, 114, 24, 9688–9689Publication Date (Print):November 1, 1992Publication History Published online1 May 2002Published inissue 1 November 1992https://pubs.acs.org/doi/10.1021/ja00050a075https://doi.org/10.1021/ja00050a075research-articleACS...
We report the discovery of a Nurr1-RXRα heterodimer-selective rexinoid which emerged from structural modification aminopyrimidine XCT0135908. Although XCT0135908 demonstrated high selectivity for heterodimer over other RXRα dimerization partners, its poor in vivo stability and limited brain penetration hindered utility. Structure–activity relationship (SAR) studies alongside bioactivity evaluations diverse series substituted pyrimidines led to BRF110, brain-penetrant compound retaining...
[reaction: see text] The radical cyclization approach to the morphine alkaloids has been applied in an asymmetric synthesis of (-)-dihydrocodeinone. A chiral cyclohexenol (R-32), from CBS reduction enone, is source chirality. first key step, tandem closure which stereochemistry controlled by geometric constraints, (-)-15b --> (+)-16, was followed unprecedented reductive hydroamination, completing (-)-dihydroisocodeine ((-)-17) 13 steps commercially available materials.
Supported ionic liquid phase (SILP) systems were prepared by immobilizing a methylimidazolium cation based onto the pore surface of two types support, MCM-41 and Vycor. The "grafting to" method was applied, involving (3-chloropropyl)-trialkoxysilane anchoring on supports' silanol groups, followed treatment with 1-methylimidazole ion exchange PF(6)(-). Optimum pretreatment procedures reaction conditions for enhanced (IL) loading properly defined applied all modifications. A study effect...
Gemcitabine, a drug with established efficacy against number of solid tumors, has therapeutic limitations due to its rapid metabolic inactivation. The aim this study was the development an innovative strategy produce metabolically stable analogue gemcitabine that could also be selectively delivered prostate cancer (CaP) cells based on cell surface expression Gonadotropin Releasing Hormone-Receptor (GnRH-R). synthesis and evaluation conjugated molecules, consisting linked GnRH agonist, is...
Naturally occurring cinnamic acid derivatives are ubiquitously distributed in the plant kingdom, and it has been proposed that their consumption contributes to maintenance of human health. However, molecular mechanisms underlying health keeping effects remain unknown. In present investigation, we evaluated capacity several (trans-cinnamic, p-coumaric, caffeic ferulic acids, as well acid-methyl -propyl esters) protect cells from oxidative stress-induced DNA damage. It was observed effective...
The potential to heighten the efficacy of antiangiogenic agents was explored in this study based on active targeting tumor cells overexpressing gonadotropin-releasing hormone receptor (GnRH-R). rational design pursued focused five analogues a clinically established compound (sunitinib), from which lead candidate (SAN1) conjugated peptide [d-Lys(6)]-GnRH, generating SAN1GSC. Conjugation SAN1 did not disrupt any its or cytotoxic properties GnRH-R-expressing prostate and breast cells. Daily...
Gemcitabine is a clinically established anticancer agent potent in various solid tumors but limited by its rapid metabolic inactivation and off-target toxicity. We have previously generated metabolically superior to gemcitabine molecule (GSG) conjugating gonadotropin releasing hormone receptor (GnRH-R) ligand peptide showed that GSG was efficacious castration resistant prostate cancer (CRPC) animal model. The current article provides an in-depth mechanistic study of GSG, coupled with...
ADVERTISEMENT RETURN TO ISSUEPREVArticleNEXTThe Radical Cyclization Approach to Morphine. Models for Highly Oxygenated Ring-III SynthonsKathlyn A. Parker and Demosthenes FokasCite this: J. Org. Chem. 1994, 59, 14, 3933–3938Publication Date (Print):July 1, 1994Publication History Published online1 May 2002Published inissue 1 July 1994https://pubs.acs.org/doi/10.1021/jo00093a027https://doi.org/10.1021/jo00093a027research-articleACS PublicationsRequest reuse permissionsArticle...
ADVERTISEMENT RETURN TO ISSUEPREVArticleNEXTStereochemistry of Radical Cyclizations to Side-Chain Olefinic Bonds. An Approach Control the C-9 Center MorphineKathlyn A. Parker and Demosthenes FokasCite this: J. Org. Chem. 1994, 59, 14, 3927–3932Publication Date (Print):July 1, 1994Publication History Published online1 May 2002Published inissue 1 July 1994https://pubs.acs.org/doi/10.1021/jo00093a026https://doi.org/10.1021/jo00093a026research-articleACS PublicationsRequest reuse...
Abstract For see ChemInform in Full Text.
Abstract A facile synthesis of 2,3,6,11-tetrahydro-1H,5H-indolizino[8,7-b]indole-11b-carboxylic acid methyl ester, a versatile intermediate utilized in the indole alkaloids, was achieved two steps. Condensation tryptamine with dimethyl α-ketoglutarate led to formation corresponding indolizino[8,7-b]indolone which subsequently underwent an efficient lactam reduction 9-BBN generate tertiary amine ester good yield. Keywords: 9-BBNDimethyl α-ketoglutaratelactam reductiontryptamine...