ArticleActa pharmacologica Sinica2012
Novel microtubule-targeted agent 6-chloro-4-(methoxyphenyl) coumarin induces G2-M arrest and apoptosis in HeLa cells.
Article in Acta pharmacologica Sinica, 2012. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 10 papers.
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Who cites it
10 citing papers in PubMed, 38 citations in OpenAlex.
- The Mechanisms of Ramulus Cinnamomi and Rhizoma Paridis in Gynecological Cancers: A Narrative Review.Cancer management and research · 2026Review
- A comprehensive review on the potential of coumarin and related derivatives as multi-target therapeutic agents in the management of gynecological cancers.Frontiers in pharmacology · 2024Review
- Synthesis and Antiproliferative Effect of Halogenated Coumarin Derivatives.Molecules (Basel, Switzerland) · 2022Article
- Allelochemical Activity of Eugenol-Derived Coumarins onPlants (Basel, Switzerland) · 2020Article
- Enhanced uptake, high selective and microtubule disrupting activity of carbohydrate fused pyrano-pyranones derived from natural coumarins attributes to its anti-malarial potential.Malaria journal · 2019Article
- Novel coumarin-6-sulfonamides as apoptotic anti-proliferative agents: synthesis, in vitro biological evaluation, and QSAR studies.Journal of enzyme inhibition and medicinal chemistry · 2018Article
- The Effect of Millisecond Pulsed Electric Fields (msPEF) on Intracellular Drug Transport with Negatively Charged Large Nanocarriers Made of Solid Lipid Nanoparticles (SLN): In Vitro Study.The Journal of membrane biology · 2016Article
- Physalin B not only inhibits the ubiquitin-proteasome pathway but also induces incomplete autophagic response in human colon cancer cells in vitro.Acta pharmacologica Sinica · 2015Article
- Identification of DW532 as a novel anti-tumor agent targeting both kinases and tubulin.Acta pharmacologica Sinica · 2014Article
- Establishing a High-content Analysis Method for Tubulin Polymerization to Evaluate Both the Stabilizing and Destabilizing Activities of Compounds.Current chemical genomics and translational medicine · 2014Article
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Authors and funding
5 authors at 2 institutions in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
aimTo identify a novel coumarin analogue with the highest anticancer activity and to further investigate its anticancer mechanisms.
methodsThe viability of cancer cells was investigated using the MTT assay. The cell cycle progression was evaluated using both flow cytometric and Western blotting analysis. Microtubule depolymerization was observed with immunocytochemistry in vivo and a tubulin depolymerization assay in vitro. Apoptosis was demonstrated using Annexin V/Propidium Iodide (PI) double-staining and sub-G(1) analysis.
resultsAmong 36 analogues of coumarin, 6-chloro-4-(methoxyphenyl) coumarin showed the best anticancer activity (IC(50) value about 200 nmol/L) in HCT116 cells. The compound had a broad spectrum of anticancer activity against 9 cancer cell lines derived from colon cancer, breast cancer, liver cancer, cervical cancer, leukemia, epidermoid cancer with IC(50) value of 75 nmol/L-1.57 μmol/L but with low cytotocitity against WI-38 human lung fibroblasts (IC(50) value of 12.128 μmol/L). The compound (0.04-10 μmol/L) induced G(2)-M phase arrest in HeLa cells in a dose-dependent manner, which was reversible after the compound was removed. The compound (10-300 μmol/L) induced the depolymerization of purified porcine tubulin in vitro. Finally, the compound (0.04-2.5 μmol/L) induced apoptosis of HeLa cells in dose- and time-dependent manners.
conclusion6-Chloro-4-(methoxyphenyl) coumarin is a novel microtubule-targeting agent that induces G(2)-M arrest and apoptosis in HeLa cells.
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