Marek Kubiszewski
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View article: Metabolic Interactions of Side-chain Extended and Unsaturated Vitamin D Analogs with Cytochrome P450 Enzymes: Integrating Theoretical and Experimental Approaches
Metabolic Interactions of Side-chain Extended and Unsaturated Vitamin D Analogs with Cytochrome P450 Enzymes: Integrating Theoretical and Experimental Approaches Open
The clinical use of 1,25-dihydroxycholecalciferol (1,25D3), the active form of vitamin D3, is limited by its calcemic side effects and rapid metabolic degradation. To overcome these limitations, we designed novel vitamin D analogs with ext…
View article: 5,7-Diiodoquinolin-8-yl (E)-3-(3,4-dihydroxyphenyl)acrylate
5,7-Diiodoquinolin-8-yl (E)-3-(3,4-dihydroxyphenyl)acrylate Open
We report the synthesis of 5,7-diiodoquinolin-8-yl ester of caffeic acid and its O,O-diallyl-protected analogue. The compounds from the hybrid class were fully characterised using NMR spectroscopy and high-resolution mass spectrometry.
View article: Preparation of Diosgenin-Functionalized Gold Nanoparticles: From Synthesis to Antitumor Activities
Preparation of Diosgenin-Functionalized Gold Nanoparticles: From Synthesis to Antitumor Activities Open
Cancer ranks among the top causes of illness and death globally. Nanotechnology holds considerable promise for enhancing the effectiveness of therapeutic and diagnostic approaches in cancer treatment. Our study presents a promising strateg…
View article: The Conjugates of Indolo[2,3-b]quinoline as Anti-Pancreatic Cancer Agents: Design, Synthesis, Molecular Docking and Biological Evaluations
The Conjugates of Indolo[2,3-b]quinoline as Anti-Pancreatic Cancer Agents: Design, Synthesis, Molecular Docking and Biological Evaluations Open
New amide conjugates of hydroxycinnamic acids (HCAs) and the known antineoplastic 5,11-dimethyl-5H-indolo[2,3-b]quinoline (DiMIQ), an analog of the natural alkaloid neocryptolepine, were synthesized and tested in vitro for anticancer activ…
View article: Experimental verification of halomethyl carbinol synthesis from carbonyl compounds using a TiCl<sub>4</sub>–Mg bimetallic complex promoter
Experimental verification of halomethyl carbinol synthesis from carbonyl compounds using a TiCl<sub>4</sub>–Mg bimetallic complex promoter Open
A mechanism for the formation of vicinal 1,2-diols in the presence of a bimetallic TiCl 4 –Mg promoter is proposed, supported by the analysis of experimental data (twelve examples) and theoretical DFT calculations (DFT/B3LYP).
View article: The conjugates of 5′-deoxy-5-fluorocytidine and hydroxycinnamic acids – synthesis, anti-pancreatic cancer activity and molecular docking studies
The conjugates of 5′-deoxy-5-fluorocytidine and hydroxycinnamic acids – synthesis, anti-pancreatic cancer activity and molecular docking studies Open
New conjugates 1–6 containing 5-dFCR and selected hydroxycinnamic acids were synthesized and tested in vitro against pancreatic cancer (PDAC) lines. The ADME properties and molecular docking to CES2 or human albumin were discussed.
View article: Efficient One-Pot Synthesis of Novel Caffeic Acid Derivatives as Potential Antimalarials
Efficient One-Pot Synthesis of Novel Caffeic Acid Derivatives as Potential Antimalarials Open
New protocol for the preparation of the novel caffeic acid derivatives using the Wittig reaction has been applied to follow the principles of green chemistry. The compounds have been evaluated against chloroquine-sensitive and chloroquine-…
View article: Synthesis, Biological Activity, ADME and Molecular Docking Studies of Novel Ursolic Acid Derivatives as Potent Anticancer Agents
Synthesis, Biological Activity, ADME and Molecular Docking Studies of Novel Ursolic Acid Derivatives as Potent Anticancer Agents Open
A series of new ursolic acid (UA) derivatives substituted with various amino acids (AAs) or dipeptides (DP) at the C-3 position of the steroid skeleton was designed and synthesized. The compounds were obtained by the esterification of UA w…
View article: Synthesis of Thiol Derivatives of Biological Active Compounds for Nanotechnology Application
Synthesis of Thiol Derivatives of Biological Active Compounds for Nanotechnology Application Open
An efficient method of thiol group introduction to the structure of common natural products and synthetic active compounds with recognized biological efficacy such genistein (1), 5,11-dimethyl-5H-indolo[2,3-b]quinolin (2), capecitabine (3)…
View article: CCDC 1952668: Experimental Crystal Structure Determination
CCDC 1952668: Experimental Crystal Structure Determination Open
An entry from the Cambridge Structural Database, the world’s repository for small molecule crystal structures. The entry contains experimental data from a crystal diffraction study. The deposited dataset for this entry is freely available …
View article: Design of Therapeutic Self-Assembled Monolayers of Thiolated Abiraterone
Design of Therapeutic Self-Assembled Monolayers of Thiolated Abiraterone Open
The aim of our work was to synthetize of a new analogue of abiraterone—thiolated abiraterone (HS-AB) and design a gold surface monolayer, bearing in mind recent advances in tuning monolayer structures and using them as efficient drug deliv…
View article: Design and Molecular Modeling of Abiraterone-Functionalized Gold Nanoparticles
Design and Molecular Modeling of Abiraterone-Functionalized Gold Nanoparticles Open
The aim of our work was the synthesis and physicochemical characterization of a unique conjugate consisting of gold nanoparticles (AuNPs) and a pharmacologically active anticancer substance abiraterone (AB). The direct coupling of AB with …
View article: CCDC 1451325: Experimental Crystal Structure Determination
CCDC 1451325: Experimental Crystal Structure Determination Open
An entry from the Cambridge Structural Database, the world’s repository for small molecule crystal structures. The entry contains experimental data from a crystal diffraction study. The deposited dataset for this entry is freely available …
View article: CCDC 1451326: Experimental Crystal Structure Determination
CCDC 1451326: Experimental Crystal Structure Determination Open
An entry from the Cambridge Structural Database, the world’s repository for small molecule crystal structures. The entry contains experimental data from a crystal diffraction study. The deposited dataset for this entry is freely available …
View article: Pemetrexed conjugated with gold nanoparticles – Synthesis, characterization and a study of noncovalent interactions
Pemetrexed conjugated with gold nanoparticles – Synthesis, characterization and a study of noncovalent interactions Open
Gold nanoparticles (AuNPs) have been widely used as nanocarriers in drug delivery application. However, the binding mechanism between AuNPs and drug bases still remains a puzzle. Our study included: (i) optimization of three synthesis of t…
View article: Synthesis and analytical characterization of gold nanoparticles for anticancer drug delivery application
Synthesis and analytical characterization of gold nanoparticles for anticancer drug delivery application Open
For many years research has been carried out to form selective drug carriers. Gold nanoparticles (AuNP) are of particular interest. New perspectives of these nanoparticles as drug carries include: the use of drugs which are poorly soluble …
View article: Synthesis and analytical characterization of gold nanoparticles for anticancer drug delivery application
Synthesis and analytical characterization of gold nanoparticles for anticancer drug delivery application Open
For many years research has been carried out to form selective drug carriers. Gold nanoparticles (AuNP) are of particular interest. New perspectives of these nanoparticles as drug carries include: the use of drugs which are poorly soluble …