ArticlePloS one2017
Structurally simplified biphenyl combretastatin A4 derivatives retain in vitro anti-cancer activity dependent on mitotic arrest.
Article in PloS one, 2017. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 12 papers.
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Who cites it
12 citing papers in PubMed, 31 citations in OpenAlex.
- New melatonin biphenyl-linked scaffold targeting colorectal cancer: design, synthesis, biological, and ADME-Tox modelling studies.RSC medicinal chemistry · 2025Article
- Design, Synthesis and Biological Evaluation of Thiazolidine-2,4-dione-biphenyl Derivatives as Anticancer Agents.Asian Pacific journal of cancer prevention : APJCP · 2025Article
- Characterization of Caerulomycin A as a dual-targeting anticancer agent.European journal of pharmacology · 2022Article
- Article
- Biphenyls in Clusiaceae: Isolation, structure diversity, synthesis and bioactivity.Frontiers in chemistry · 2022Review
- New Heterocyclic Combretastatin A-4 Analogs: Synthesis and Biological Activity of Styryl-2(3Pharmaceuticals (Basel, Switzerland) · 2021Article
- Discovery of novel quinoline-based analogues of combretastatin A-4 as tubulin polymerisation inhibitors with apoptosis inducing activity and potent anticancer effect.Journal of enzyme inhibition and medicinal chemistry · 2021Article
- Antiproliferative and antiinflammatory coxib-combretastatin hybrids suppress cell cycle progression and induce apoptosis of MCF7 breast cancer cells.Molecular diversity · 2021Article
- Design, synthesis and biological evaluation of combretastatin A-4 sulfamate derivatives as potential anti-cancer agents.RSC medicinal chemistry · 2021Article
- RETRACTED: Potent Quinoline-Containing Combretastatin A-4 Analogues: Design, Synthesis, Antiproliferative, and Anti-Tubulin Activity.Pharmaceuticals (Basel, Switzerland) · 2020Article
- Antitumor Drug Combretastatin-A4 Phosphate Aggravates the Symptoms of Dextran Sulfate Sodium-Induced Ulcerative Colitis in Mice.Frontiers in pharmacology · 2020Article
- Deciphering the origins of molecular toxicity of combretastatin A4 and its glycoconjugates: interactions with major drug transporters and their safety profilesMedChemComm · 2017Article
Corrections and comments
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Authors and funding
9 authors at 2 institutions in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
The cis-stilbene, combretastatin A4 (CA4), is a potent microtubule targeting and vascular damaging agent. Despite promising results at the pre-clinical level and extensive clinical evaluation, CA4 has yet to be approved for therapeutic use. One impediment to the development of CA4 is an inherent conformational instability about the ethylene linker, which joins two aromatic rings. We have previously published preliminary data regarding structurally simplified biphenyl derivatives of CA4, lacking an ethylene linker, which retain anti-proliferative and pro-apoptotic activity, albeit at higher doses. Our current study provides a more comprehensive evaluation regarding the anti-proliferative and pro-apoptotic properties of biphenyl CA4 derivatives in both 2D and 3D cancerous and non-cancerous cell models. Computational analysis has revealed that cytotoxicity of CA4 and biphenyl analogues correlates with predicted tubulin affinity. Additional mechanistic evaluation of the biphenyl derivatives found that their anti-cancer activity is dependent on prolonged mitotic arrest, in a similar manner to CA4. Lastly, we have shown that cancer cells deficient in the extrinsic pathway of apoptosis experience delayed cell death following treatment with CA4 or analogues. Biphenyl derivatives of CA4 represent structurally simplified analogues of CA4, which retain a similar mechanism of action. The biphenyl analogues warrant in vivo examination to evaluate their potential as vascular damaging agents.
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