Journal: British Journal of Cancer

Article Title: In vivo and in vitro properties of STX2484: a novel non-steroidal anti-cancer compound active in taxane-resistant breast cancer

doi: 10.1038/bjc.2014.188

Figure Lengend Snippet: Microtubule disruption. ( A ) Microtubule polymerisation assay. Tubulin assembly was measured by changes in turbidity. Tubulin was incubated with 10 μ M paclitaxel or GTP in the presence or absence of 10 μ M STX2484 at 37 °C. The change in absorbance was continuously monitored at 350 nm for 40 min. For competitive-colchicine-binding site studies, STX2484 was tested at 10 μ M and the reference compounds paclitaxel and colchicine were tested at 10 μ M . Each point represents the mean±s.d. of three independent experiments. ( B ) Fluorescent images of MCF-7 and MDA-MB-231 cells after drug exposure. Cells were treated for 24 h with 0.1 μ M STX2484 and stained with FITC-conjugated anti-tubulin antibody (tubulin) and Hoechst (nucleus). This low dose, compared with IC 50 values, was used to observe STX2484 effect on the cytoskeleton without killing the cells. Images were taken using a Zeiss inverted microscope under × 200 magnification.

Article Snippet: The polymerisation of purified bovine brain tubulin (99% purity) was monitored using the Tubulin Polymerization Assay Kit from CytoDYNAMIX (Screen 03, Cytoskeleton Inc., Denver, CO, USA; Shelanski et al , 1973 ; ).

Techniques: Incubation, Binding Assay, Staining, Inverted Microscopy

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