article · Pharmaceuticals
A series of novel thiazole-based chalcones were evaluated for their anticancer activity as potential tubulin polymerization inhibitors. In vitro anticancer screening for the thiazole derivatives <b>2a</b>-<b>2p</b> exhibited broad-spectrum antitumor activity against various cancer cell lines particularly Ovar-3 and MDA-MB-468 cells with a GI<sub>50</sub> range from 1.55 to 2.95 μΜ, respectively. Compound <b>2e</b> demonstrated significant inhibition of tubulin polymerization, with an IC<sub>50</sub> value of 7.78 μM compared to Combretastatin-A4 (CA-4), with an IC<sub>50</sub> value of 4.93 μM. Molecular docking studies of compounds <b>2e</b>, <b>2g</b>, and <b>2h</b> into tubulin further supported these findings, revealing that they bind effectively to the colchicine binding site, mirroring key interactions exhibited by CA-4. Computational predictions suggested favorable oral bioavailability and drug-likeness for these compounds, highlighting their potential for further development as chemotherapeutic agents.
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DOI: 10.3390/ph17091154
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