Journal: RSC Advances

Article Title: Design, synthesis, and mechanistic evaluation of novel pyrazole/thiazole chalcone hybrids as dual tubulin polymerization and COX-2 inhibitors with potent antiproliferative activity

doi: 10.1039/d6ra03557d

Figure Lengend Snippet: Selected thiazole/chalcone-based tubulin polymerization inhibitors (I–VII) and combretastatin A-4.

Article Snippet: The effects of compounds 9a–o on tubulin polymerization were assessed using a fluorescence-based tubulin polymerization assay (Cytoskeleton, Inc., Cat. No. BK011P), with combretastatin A-4 as the reference inhibitor.

Techniques:

Journal: RSC Advances

Article Title: Design, synthesis, and mechanistic evaluation of novel pyrazole/thiazole chalcone hybrids as dual tubulin polymerization and COX-2 inhibitors with potent antiproliferative activity

doi: 10.1039/d6ra03557d

Figure Lengend Snippet: Tubulin polymerization inhibitory activity of compounds 9a–o and the reference inhibitor CA-4, expressed as IC 50 values (µM), as determined from a fluorescence-based polymerization assay monitored kinetically for 60 min at 37 °C. Data are presented as mean ± SEM.

Article Snippet: The effects of compounds 9a–o on tubulin polymerization were assessed using a fluorescence-based tubulin polymerization assay (Cytoskeleton, Inc., Cat. No. BK011P), with combretastatin A-4 as the reference inhibitor.

Techniques: Activity Assay, Fluorescence, Polymerization Assay

Journal: RSC Advances

Article Title: Design, synthesis, and mechanistic evaluation of novel pyrazole/thiazole chalcone hybrids as dual tubulin polymerization and COX-2 inhibitors with potent antiproliferative activity

doi: 10.1039/d6ra03557d

Figure Lengend Snippet: Superimposition of the co-crystallized (green) and redocked (brown) colchicine poses within the colchicine-binding site of tubulin (PDB ID: 4O2B).

Article Snippet: The effects of compounds 9a–o on tubulin polymerization were assessed using a fluorescence-based tubulin polymerization assay (Cytoskeleton, Inc., Cat. No. BK011P), with combretastatin A-4 as the reference inhibitor.

Techniques: Binding Assay

Journal: RSC Advances

Article Title: Design, synthesis, and mechanistic evaluation of novel pyrazole/thiazole chalcone hybrids as dual tubulin polymerization and COX-2 inhibitors with potent antiproliferative activity

doi: 10.1039/d6ra03557d

Figure Lengend Snippet: Binding interactions of compound 9l within the colchicine-binding site of tubulin (PDB ID: 4O2B): (A) 2D interaction diagram and (B) 3D binding mode.

Article Snippet: The effects of compounds 9a–o on tubulin polymerization were assessed using a fluorescence-based tubulin polymerization assay (Cytoskeleton, Inc., Cat. No. BK011P), with combretastatin A-4 as the reference inhibitor.

Techniques: Binding Assay

Journal: PLoS ONE

Article Title: Docking, Synthesis and Antiproliferative Activity of N -Acylhydrazone Derivatives Designed as Combretastatin A4 Analogues

doi: 10.1371/journal.pone.0085380

Figure Lengend Snippet: Polar interactions between CA-4 (A) or LASSBio-1593 (B) with the colchicine binding site of β-tubulin (PDB code: 1sa0).

Article Snippet: The tubulin polymerization assay was performed by CEREP® employing a single concentration of 5b (C = 30 μM), using vinblastine as positive control.

Techniques: Binding Assay

Journal: PLoS ONE

Article Title: Docking, Synthesis and Antiproliferative Activity of N -Acylhydrazone Derivatives Designed as Combretastatin A4 Analogues

doi: 10.1371/journal.pone.0085380

Figure Lengend Snippet: Scores estimated by molecular docking (ChemScore fitness function) for colchicine binding site of β-tubulin, cLogP, cLogD 7.0 , molar refractivity and the aqueous solubility of CA-4 and its N -acylhydrazone analogues 5a–r .

Article Snippet: The tubulin polymerization assay was performed by CEREP® employing a single concentration of 5b (C = 30 μM), using vinblastine as positive control.

Techniques: Binding Assay, Solubility, Analogues

Journal: PLoS ONE

Article Title: Docking, Synthesis and Antiproliferative Activity of N -Acylhydrazone Derivatives Designed as Combretastatin A4 Analogues

doi: 10.1371/journal.pone.0085380

Figure Lengend Snippet: Best poses of compounds 5b (A), 10 (B), 9 (C) and 12 (D) at the colchicine binding pocket β-tubulin (PDB code: 1sa0).

Article Snippet: The tubulin polymerization assay was performed by CEREP® employing a single concentration of 5b (C = 30 μM), using vinblastine as positive control.

Techniques: Binding Assay