Development of a Novel Series of Thiazole-Based Tubulin Polymerization Inhibitors

A research document detailing the synthesis and biological evaluation of 15 novel thiazole-based compounds (8a-o) as potential anticancer agents. The study, authored by Lamya H. Al-Wahaibi and last updated in April 2026, includes results from single-dose and five-dose antiproliferative assays against the NCI 60 cell line panel, tubulin inhibition IC50 values, cell cycle analysis, and molecular docking studies. The data is shared under a CC-BY-4.0 license.

Use Cases

• Training predictive models for compound activity based on the reported GI50, TGI, and LC50 values across 60 cell lines.
• Benchmarking new tubulin inhibitors against the reported IC50 values (3.86 to 7.19 µM) for compounds 8b, 8d, and 8m.
• Analyzing structure-activity relationships for thiazole-based compounds using the described molecular docking results at the colchicine site.
• Studying mechanisms of G2/M phase cell cycle arrest using the reported increase from 13.74% to 45.35% in MCF-7 cells.

Strengths

• Includes specific, quantitative biological results for 15 compounds, including GI50, TGI, LC50, and tubulin inhibition IC50 values.
• Provides mechanistic validation through cell cycle analysis (G2/M arrest) and Western blot results showing decreased tubulin expression.
• Contains in silico ADMET profiling and molecular docking data for compound 8m, suggesting a promising drug-like profile.

Limitations

• The primary data file is a 21.0 MB DOCX document; the underlying structured data (e.g., raw assay results) is not directly accessible as a dataset.
• Column-level documentation is absent; field semantics must be inferred from the textual description after download.
• Row count is unknown, which may limit suitability assessment for direct computational analysis.

Provenance

Source

figshare

Collection Method

Experimental synthesis and biological evaluation as described in the document.

Time Range

The study period is not specified; the document was last updated in April 2026.

Freshness

Last updated 2026-04-22 05:46:15; freshness should be verified.

Geography

Spatial coverage is not specified.