AI Article Synopsis
- - A new series of thiazole-based chalcones was tested for anticancer properties, showing effective inhibition of cancer cell growth, particularly in Ovar-3 and MDA-MB-468 cells, at concentrations between 1.55 and 2.95 μM.
- - One compound notably inhibited tubulin polymerization with an IC value of 7.78 μM, which is less effective than the reference drug Combretastatin-A4 (CA-4) at 4.93 μM.
- - Molecular docking studies indicated that these compounds effectively bind to the same site on tubulin as CA-4, along with predictions suggesting they have good oral bioavailability and potential as chemotherapy drugs.
Article Abstract
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 - exhibited broad-spectrum antitumor activity against various cancer cell lines particularly Ovar-3 and MDA-MB-468 cells with a GI range from 1.55 to 2.95 μΜ, respectively. Compound demonstrated significant inhibition of tubulin polymerization, with an IC value of 7.78 μM compared to Combretastatin-A4 (CA-4), with an IC value of 4.93 μM. Molecular docking studies of compounds , , and 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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Source |
|---|---|
| http://www.ncbi.nlm.nih.gov/pmc/articles/PMC11435058 | PMC |
| http://dx.doi.org/10.3390/ph17091154 | DOI Listing |
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