AI Article Synopsis
- A new class of compounds based on rhodanine and 4-anilinoquinazoline was designed by combining quinazoline with various rhodanine groups.
- These compounds were tested for their ability to inhibit cell growth (antiproliferative activity) and showed promising results, particularly in blocking the activity of EGFR-TK.
- Specifically, compound 8d exhibited strong inhibitory effects with low IC50 values against liver cancer (Hep G2) and lung cancer (A549) cell lines, and molecular docking suggested that its structure fits well in the EGFR TK active site, explaining its effectiveness.
Article Abstract
A type of novel rhodanine-based 4-anilinoquinazoline, which designed the combination between quinazoline as the backbone and various substituted biological rhodanine groups as the side chain, have been synthesized, and their antiproliferative activities were also evaluated firstly. These compounds displayed good antiproliferative activity and EGFR-TK inhibitory activity. Among them, compound 8d showed good inhibitory activity (IC50=2.7μM for Hep G2, IC50=3.1μM for A549) and molecular docking of 8d into EGFR TK active site was also performed, this inhibitor well fitting the active site might well explain its excellent inhibitory activity.
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| http://dx.doi.org/10.1016/j.bmc.2015.04.065 | DOI Listing |
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