AI Article Synopsis
- A series of derivatives of the compound withangulatin A (WA) were created and tested for their effectiveness against four types of human cancer cells.
- Among these derivatives, one compound (referred to as 10) was found to be highly effective, showing an IC value of 74.0 nM against the breast cancer cell line MDA-MB-231, significantly outperforming WA itself.
- Compound 10 not only arrested cancer cells in the G2 phase of the cell cycle but also triggered apoptosis by increasing levels of reactive oxygen species (ROS), demonstrating strong selectivity for the targeted cancer cells with a high selectivity index.
Article Abstract
Novel withangulatin A (WA) derivatives were synthesized and evaluated for antiproliferative activity against four human cancer cell lines (U2OS, MDA-MB-231, HepG2, and A549). Among these derivatives, 10 exhibited the most potent antiproliferative activity, with an IC value of 74.0 nM against the human breast cancer cell line MDA-MB-231 and potency that was 70-fold that of WA (IC = 5.22 µM). Moreover, 10 caused G2-phase cell cycle arrest in a concentration-dependent manner and induced the apoptosis of MDA-MB-231 cells by increasing intracellular reactive oxygen species (ROS). Compound 10 showed a high selectivity index (SI = 267.03) for breast cancer MDA-MB-231 cells. These results suggest that 10 is a promising anticancer agent.
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| http://dx.doi.org/10.1016/j.bioorg.2021.104690 | DOI Listing |
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Article Synopsis
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