Journal: Pharmaceuticals

Article Title: Synthesis and Evaluation of Some New 4 H -Pyran Derivatives as Antioxidant, Antibacterial and Anti-HCT-116 Cells of CRC, with Molecular Docking, Antiproliferative, Apoptotic and ADME Investigations

doi: 10.3390/ph15070891

Figure Lengend Snippet: Examples of pyran-containing compounds with antibacterial , antioxidant and anticancer activities via inhibition of CDK2 [ , , ].

Article Snippet: The in vitro quantitative measurement of concentration of CDK2 in lysates of HCT-116 cells was carried out using a commercial Human CDK2 ELISA Kit (cat. no.: LS-F22176; LifeSpan Biosciences Inc., Seattle, WA, USA) in the presence or absence of the studied compounds ( 4d and 4k ), following the manufacturer’s instructions.

Techniques: Inhibition

Journal: Pharmaceuticals

Article Title: Synthesis and Evaluation of Some New 4 H -Pyran Derivatives as Antioxidant, Antibacterial and Anti-HCT-116 Cells of CRC, with Molecular Docking, Antiproliferative, Apoptotic and ADME Investigations

doi: 10.3390/ph15070891

Figure Lengend Snippet: Redocked (yellow) and co-crystallized (baby blue) ligand ( DTQ ) in the ATP binding pocket of CDK2 after self-docking calculations.

Article Snippet: The in vitro quantitative measurement of concentration of CDK2 in lysates of HCT-116 cells was carried out using a commercial Human CDK2 ELISA Kit (cat. no.: LS-F22176; LifeSpan Biosciences Inc., Seattle, WA, USA) in the presence or absence of the studied compounds ( 4d and 4k ), following the manufacturer’s instructions.

Techniques: Binding Assay

Journal: Pharmaceuticals

Article Title: Synthesis and Evaluation of Some New 4 H -Pyran Derivatives as Antioxidant, Antibacterial and Anti-HCT-116 Cells of CRC, with Molecular Docking, Antiproliferative, Apoptotic and ADME Investigations

doi: 10.3390/ph15070891

Figure Lengend Snippet: Binding free energy of 4d , 4k , 4f , BMS-265246 and DTQ at the active site of CDK2.

Article Snippet: The in vitro quantitative measurement of concentration of CDK2 in lysates of HCT-116 cells was carried out using a commercial Human CDK2 ELISA Kit (cat. no.: LS-F22176; LifeSpan Biosciences Inc., Seattle, WA, USA) in the presence or absence of the studied compounds ( 4d and 4k ), following the manufacturer’s instructions.

Techniques: Binding Assay

Journal: Pharmaceuticals

Article Title: Synthesis and Evaluation of Some New 4 H -Pyran Derivatives as Antioxidant, Antibacterial and Anti-HCT-116 Cells of CRC, with Molecular Docking, Antiproliferative, Apoptotic and ADME Investigations

doi: 10.3390/ph15070891

Figure Lengend Snippet: Three-dimensional binding interactions of DTQ within the ATP binding pocket of CDK2. Hydrogen bonds (yellow dotted lines), hydrogen atoms (white), nitrogen atoms (blue), and oxygen atoms (red).

Article Snippet: The in vitro quantitative measurement of concentration of CDK2 in lysates of HCT-116 cells was carried out using a commercial Human CDK2 ELISA Kit (cat. no.: LS-F22176; LifeSpan Biosciences Inc., Seattle, WA, USA) in the presence or absence of the studied compounds ( 4d and 4k ), following the manufacturer’s instructions.

Techniques: Binding Assay

Journal: Pharmaceuticals

Article Title: Synthesis and Evaluation of Some New 4 H -Pyran Derivatives as Antioxidant, Antibacterial and Anti-HCT-116 Cells of CRC, with Molecular Docking, Antiproliferative, Apoptotic and ADME Investigations

doi: 10.3390/ph15070891

Figure Lengend Snippet: Two-dimensional binding interactions of DTQ within the ATP binding pocket of CDK2.

Article Snippet: The in vitro quantitative measurement of concentration of CDK2 in lysates of HCT-116 cells was carried out using a commercial Human CDK2 ELISA Kit (cat. no.: LS-F22176; LifeSpan Biosciences Inc., Seattle, WA, USA) in the presence or absence of the studied compounds ( 4d and 4k ), following the manufacturer’s instructions.

Techniques: Binding Assay

Journal: Pharmaceuticals

Article Title: Synthesis and Evaluation of Some New 4 H -Pyran Derivatives as Antioxidant, Antibacterial and Anti-HCT-116 Cells of CRC, with Molecular Docking, Antiproliferative, Apoptotic and ADME Investigations

doi: 10.3390/ph15070891

Figure Lengend Snippet: Three-dimensional binding interactions of BMS-265246 within the ATP binding pocket of CDK2. Hydrogen bond (purple dotted line), hydrogen atoms (white), nitrogen atoms (blue), fluorine atoms (light green), and oxygen atoms (red).

Article Snippet: The in vitro quantitative measurement of concentration of CDK2 in lysates of HCT-116 cells was carried out using a commercial Human CDK2 ELISA Kit (cat. no.: LS-F22176; LifeSpan Biosciences Inc., Seattle, WA, USA) in the presence or absence of the studied compounds ( 4d and 4k ), following the manufacturer’s instructions.

Techniques: Binding Assay

Journal: Pharmaceuticals

Article Title: Synthesis and Evaluation of Some New 4 H -Pyran Derivatives as Antioxidant, Antibacterial and Anti-HCT-116 Cells of CRC, with Molecular Docking, Antiproliferative, Apoptotic and ADME Investigations

doi: 10.3390/ph15070891

Figure Lengend Snippet: Two-dimensional interactions of BMS-265246 within the ATP binding pocket of CDK2 kinase.

Article Snippet: The in vitro quantitative measurement of concentration of CDK2 in lysates of HCT-116 cells was carried out using a commercial Human CDK2 ELISA Kit (cat. no.: LS-F22176; LifeSpan Biosciences Inc., Seattle, WA, USA) in the presence or absence of the studied compounds ( 4d and 4k ), following the manufacturer’s instructions.

Techniques: Binding Assay

Journal: Pharmaceuticals

Article Title: Synthesis and Evaluation of Some New 4 H -Pyran Derivatives as Antioxidant, Antibacterial and Anti-HCT-116 Cells of CRC, with Molecular Docking, Antiproliferative, Apoptotic and ADME Investigations

doi: 10.3390/ph15070891

Figure Lengend Snippet: Three-dimensional model of binding interactions of compound 4d after docking calculations in the ATP binding pocket of CDK2. Hydrogen bond (black lines), hydrogen atoms (white), nitrogen atoms (blue), and oxygen atoms (red).

Article Snippet: The in vitro quantitative measurement of concentration of CDK2 in lysates of HCT-116 cells was carried out using a commercial Human CDK2 ELISA Kit (cat. no.: LS-F22176; LifeSpan Biosciences Inc., Seattle, WA, USA) in the presence or absence of the studied compounds ( 4d and 4k ), following the manufacturer’s instructions.

Techniques: Binding Assay

Journal: Pharmaceuticals

Article Title: Synthesis and Evaluation of Some New 4 H -Pyran Derivatives as Antioxidant, Antibacterial and Anti-HCT-116 Cells of CRC, with Molecular Docking, Antiproliferative, Apoptotic and ADME Investigations

doi: 10.3390/ph15070891

Figure Lengend Snippet: Two-dimensional model of binding interactions of compound 4d after docking calculations in the ATP binding pocket of CDK2.

Article Snippet: The in vitro quantitative measurement of concentration of CDK2 in lysates of HCT-116 cells was carried out using a commercial Human CDK2 ELISA Kit (cat. no.: LS-F22176; LifeSpan Biosciences Inc., Seattle, WA, USA) in the presence or absence of the studied compounds ( 4d and 4k ), following the manufacturer’s instructions.

Techniques: Binding Assay

Journal: Pharmaceuticals

Article Title: Synthesis and Evaluation of Some New 4 H -Pyran Derivatives as Antioxidant, Antibacterial and Anti-HCT-116 Cells of CRC, with Molecular Docking, Antiproliferative, Apoptotic and ADME Investigations

doi: 10.3390/ph15070891

Figure Lengend Snippet: Three-dimensional model of binding interactions of compound 4K after docking calculations in the ATP binding pocket of CDK2. Hydrogen bond (black lines), hydrogen atoms (white), nitrogen atoms (blue), and oxygen atoms (red).

Article Snippet: The in vitro quantitative measurement of concentration of CDK2 in lysates of HCT-116 cells was carried out using a commercial Human CDK2 ELISA Kit (cat. no.: LS-F22176; LifeSpan Biosciences Inc., Seattle, WA, USA) in the presence or absence of the studied compounds ( 4d and 4k ), following the manufacturer’s instructions.

Techniques: Binding Assay

Journal: Pharmaceuticals

Article Title: Synthesis and Evaluation of Some New 4 H -Pyran Derivatives as Antioxidant, Antibacterial and Anti-HCT-116 Cells of CRC, with Molecular Docking, Antiproliferative, Apoptotic and ADME Investigations

doi: 10.3390/ph15070891

Figure Lengend Snippet: Two-dimensional model of binding interactions of compound 4K after docking calculations in the ATP binding pocket of CDK2.

Article Snippet: The in vitro quantitative measurement of concentration of CDK2 in lysates of HCT-116 cells was carried out using a commercial Human CDK2 ELISA Kit (cat. no.: LS-F22176; LifeSpan Biosciences Inc., Seattle, WA, USA) in the presence or absence of the studied compounds ( 4d and 4k ), following the manufacturer’s instructions.

Techniques: Binding Assay

Journal: Pharmaceuticals

Article Title: Synthesis and Evaluation of Some New 4 H -Pyran Derivatives as Antioxidant, Antibacterial and Anti-HCT-116 Cells of CRC, with Molecular Docking, Antiproliferative, Apoptotic and ADME Investigations

doi: 10.3390/ph15070891

Figure Lengend Snippet: Three-dimensional model of binding interactions of compound 4f after docking calculations in the ATP binding pocket of CDK2. Hydrogen atoms (white), nitrogen atoms (blue), chlorine atom (green), and oxygen atoms (red).

Article Snippet: The in vitro quantitative measurement of concentration of CDK2 in lysates of HCT-116 cells was carried out using a commercial Human CDK2 ELISA Kit (cat. no.: LS-F22176; LifeSpan Biosciences Inc., Seattle, WA, USA) in the presence or absence of the studied compounds ( 4d and 4k ), following the manufacturer’s instructions.

Techniques: Binding Assay

Journal: Pharmaceuticals

Article Title: Synthesis and Evaluation of Some New 4 H -Pyran Derivatives as Antioxidant, Antibacterial and Anti-HCT-116 Cells of CRC, with Molecular Docking, Antiproliferative, Apoptotic and ADME Investigations

doi: 10.3390/ph15070891

Figure Lengend Snippet: Two-dimensional model of binding interactions of compound 4f after docking calculations in the ATP binding pocket of CDK2.

Article Snippet: The in vitro quantitative measurement of concentration of CDK2 in lysates of HCT-116 cells was carried out using a commercial Human CDK2 ELISA Kit (cat. no.: LS-F22176; LifeSpan Biosciences Inc., Seattle, WA, USA) in the presence or absence of the studied compounds ( 4d and 4k ), following the manufacturer’s instructions.

Techniques: Binding Assay

Journal: Pharmaceuticals

Article Title: Synthesis and Evaluation of Some New 4 H -Pyran Derivatives as Antioxidant, Antibacterial and Anti-HCT-116 Cells of CRC, with Molecular Docking, Antiproliferative, Apoptotic and ADME Investigations

doi: 10.3390/ph15070891

Figure Lengend Snippet: In vitro evaluation of the CDK2 inhibitory efficiency of pyrans 4d and 4K as compared to the reference inhibitor BMS-265246 over a concentration range of 0.01−10 µM. Results were obtained from three independent experiments.

Article Snippet: The in vitro quantitative measurement of concentration of CDK2 in lysates of HCT-116 cells was carried out using a commercial Human CDK2 ELISA Kit (cat. no.: LS-F22176; LifeSpan Biosciences Inc., Seattle, WA, USA) in the presence or absence of the studied compounds ( 4d and 4k ), following the manufacturer’s instructions.

Techniques: In Vitro, Concentration Assay

Journal: Pharmaceuticals

Article Title: Synthesis and Evaluation of Some New 4 H -Pyran Derivatives as Antioxidant, Antibacterial and Anti-HCT-116 Cells of CRC, with Molecular Docking, Antiproliferative, Apoptotic and ADME Investigations

doi: 10.3390/ph15070891

Figure Lengend Snippet: IC 50 values of 4d , 4K and BMS-265246 against CDK2.

Article Snippet: The in vitro quantitative measurement of concentration of CDK2 in lysates of HCT-116 cells was carried out using a commercial Human CDK2 ELISA Kit (cat. no.: LS-F22176; LifeSpan Biosciences Inc., Seattle, WA, USA) in the presence or absence of the studied compounds ( 4d and 4k ), following the manufacturer’s instructions.

Techniques:

Journal: Pharmaceuticals

Article Title: Synthesis and Evaluation of Some New 4 H -Pyran Derivatives as Antioxidant, Antibacterial and Anti-HCT-116 Cells of CRC, with Molecular Docking, Antiproliferative, Apoptotic and ADME Investigations

doi: 10.3390/ph15070891

Figure Lengend Snippet: In vitro quantitative determination of the concentrations of CDK2 (ng/mL) in HCT116 cells treated with pyrans 4d and 4K compared with the positive control BMS-265246 and the negative control samples.

Article Snippet: The in vitro quantitative measurement of concentration of CDK2 in lysates of HCT-116 cells was carried out using a commercial Human CDK2 ELISA Kit (cat. no.: LS-F22176; LifeSpan Biosciences Inc., Seattle, WA, USA) in the presence or absence of the studied compounds ( 4d and 4k ), following the manufacturer’s instructions.

Techniques: In Vitro, Positive Control, Negative Control

Journal: Pharmaceuticals

Article Title: Synthesis and Evaluation of Some New 4 H -Pyran Derivatives as Antioxidant, Antibacterial and Anti-HCT-116 Cells of CRC, with Molecular Docking, Antiproliferative, Apoptotic and ADME Investigations

doi: 10.3390/ph15070891

Figure Lengend Snippet: The expression profiles of the CDK2 gene in the lysate of HCT-116 cancer cells treated with compounds 4d and 4 k .

Article Snippet: The in vitro quantitative measurement of concentration of CDK2 in lysates of HCT-116 cells was carried out using a commercial Human CDK2 ELISA Kit (cat. no.: LS-F22176; LifeSpan Biosciences Inc., Seattle, WA, USA) in the presence or absence of the studied compounds ( 4d and 4k ), following the manufacturer’s instructions.

Techniques: Expressing