Marcin Cybulski
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View article: Synthetic Flozins in Cancer Prevention and Combination Strategies: Structural Insights and Therapeutic Potential
Synthetic Flozins in Cancer Prevention and Combination Strategies: Structural Insights and Therapeutic Potential Open
The growing number of cancer cases highlights the urgent need to develop new therapies based on effective molecules. Although anticancer activity remains a key element of oncological pharmacology, the importance of agents that support phys…
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: Ansa–Ferrocene Derivatives as Potential Therapeutics
Ansa–Ferrocene Derivatives as Potential Therapeutics Open
It has been known since the 1990s that the introduction of a ferrocenyl–type substituent into compounds with proven biological activity can improve their properties. More recently, it was also shown that a carbon bridge connecting the two …
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: CCDC 2243270: Experimental Crystal Structure Determination
CCDC 2243270: 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: 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: Structure-Activity Relationship of Hydroxycinnamic Acid Derivatives for Cooperating with Carnosic Acid and Calcitriol in Acute Myeloid Leukemia Cells
Structure-Activity Relationship of Hydroxycinnamic Acid Derivatives for Cooperating with Carnosic Acid and Calcitriol in Acute Myeloid Leukemia Cells Open
Plant phenolic compounds have shown the ability to cooperate with one another at low doses in producing enhanced anticancer effects. This may overcome the limitations (e.g., poor bioavailability and high-dose toxicity) in developing these …
View article: Evaluation of the In Vitro Cytotoxic Activity of Caffeic Acid Derivatives and Liposomal Formulation against Pancreatic Cancer Cell Lines
Evaluation of the In Vitro Cytotoxic Activity of Caffeic Acid Derivatives and Liposomal Formulation against Pancreatic Cancer Cell Lines Open
Pancreatic cancer belongs to the most aggressive group of cancers, with very poor prognosis. Therefore, there is an important need to find more potent drugs that could deliver an improved therapeutic approach. In the current study we searc…
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: Synergistic Cytotoxicity of Methyl 4-Hydroxycinnamate and Carnosic Acid to Acute Myeloid Leukemia Cells via Calcium-Dependent Apoptosis Induction
Synergistic Cytotoxicity of Methyl 4-Hydroxycinnamate and Carnosic Acid to Acute Myeloid Leukemia Cells via Calcium-Dependent Apoptosis Induction Open
Acute myeloid leukemia (AML) is a malignant hematopoietic disease with poor prognosis for most patients. Conventional chemotherapy has been the standard treatment approach for AML in the past 40 years with limited success. Although, severa…
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: Synthesis and Antioxidant Activity of Caffeic Acid Derivatives
Synthesis and Antioxidant Activity of Caffeic Acid Derivatives Open
A series of caffeic acid derivatives were synthesized via a modified Wittig reaction which is a very important tool in organic chemistry for the construction of unsaturated carbon–carbon bonds. All reactions were performed in water medium …
View article: CCDC 802025: Experimental Crystal Structure Determination
CCDC 802025: 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 …