ArticleScientific reports2017
Novel quinolone chalcones targeting colchicine-binding pocket kill multidrug-resistant cancer cells by inhibiting tubulin activity and MRP1 function.
Article in Scientific reports, 2017. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 25 papers.
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25 citing papers in PubMed, 74 citations in OpenAlex.
- Disruption of plant cell division by methoxychalcones and cinnamaldehyde: insights into their herbicidal mode of action.Scientific reports · 2026Article
- Novel 4-quinolone derivative inflicted cytotoxicity via intrinsic apoptotic pathway activation on human metastatic triple-negative breast cancer cells.Bioorganic chemistry · 2025Article
- Amide linked chalcone derivatives, a promising class of compounds with versatile biological effects.RSC advances · 2025Review
- Acridine-Based Chalcone 1C and ABC Transporters.International journal of molecular sciences · 2025Article
- Pharmacological potential of natural chalcones: a recent studies and future perspective.Frontiers in pharmacology · 2025Review
- Quinolone Derivatives as Anticancer Agents: Importance in Medicinal Chemistry.Current topics in medicinal chemistry · 2024Review
- Natural Chalcones and Derivatives in Colon Cancer: Pre-Clinical Challenges and the Promise of Chalcone-Based Nanoparticles.Pharmaceutics · 2023Review
- Magic bullets, magic shields, and antimicrobials in between.Pharmaceutical science advances · 2023Review
- Synthesis and bioactive evaluation ofRSC medicinal chemistry · 2023Article
- A review on synthetic chalcone derivatives as tubulin polymerisation inhibitors.Journal of enzyme inhibition and medicinal chemistry · 2022Review
- Tetrahydroquinolinone derivatives exert antiproliferative effect on lung cancer cells through apoptosis induction.Scientific reports · 2022Article
- Two Important Anticancer Mechanisms of Natural and Synthetic Chalcones.International journal of molecular sciences · 2022Review
- Synthesis and Antiproliferative Activity of Novel Dehydroabietic Acid-Chalcone Hybrids.Molecules (Basel, Switzerland) · 2022Article
- Computational-Based Discovery of the Anti-Cancer Activities of Pyrrole-Based Compounds Targeting the Colchicine-Binding Site of Tubulin.Molecules (Basel, Switzerland) · 2022Article
- Novel chalcone-derived pyrazoles as potential therapeutic agents for the treatment of non-small cell lung cancer.Scientific reports · 2022Article
- Lead optimization of novel quinolone chalcone compounds by a structure-activity relationship (SAR) study to increase efficacy and metabolic stability.Scientific reports · 2021Article
- Chalcone Derivatives: Role in Anticancer Therapy.Biomolecules · 2021Review
- LMTK3 inhibition affects microtubule stability.Molecular cancer · 2021Article
- 4'-O-Methylbroussochalcone B as a novel tubulin polymerization inhibitor suppressed the proliferation and migration of acute myeloid leukaemia cells.BMC cancer · 2021Article
- Synthesis, biological evaluation, and molecular modelling of new naphthalene-chalcone derivatives as potential anticancer agents on MCF-7 breast cancer cells by targeting tubulin colchicine binding site.Journal of enzyme inhibition and medicinal chemistry · 2020Article
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Authors and funding
7 authors at 3 institutions in 2 countries.
Funding
No grant is acknowledged in the PubMed record.
Abstract
Agents targeting colchicine-binding pocket usually show a minimal drug-resistance issue, albeit often associated with high toxicity. Chalcone-based compounds, which may bind to colchicine-binding site, are found in many edible fruits, suggesting that they can be effective drugs with less toxicity. Therefore, we synthesized and examined 24 quinolone chalcone compounds, from which we identified ((E)-3-(3-(2-Methoxyphenyl)-3-oxoprop-1-enyl) quinolin-2(1H)-one) (CTR-17) and ((E)-6-Methoxy-3-(3-(2-methoxyphenyl)-3-oxoprop-1-enyl) quinolin-2(1H)-one) (CTR-20) as promising leads. In particular, CTR-20 was effective against 65 different cancer cell lines originated from 12 different tissues, largely in a cancer cell-specific manner. We found that both CTR-17 and CTR-20 reversibly bind to the colchicine-binding pocket on β-tubulin. Interestingly however, both the CTRs were highly effective against multidrug-resistant cancer cells while colchicine, paclitaxel and vinblastine were not. Our study with CTR-20 showed that it overcomes multidrug-resistance through its ability to impede MRP1 function while maintaining strong inhibition against microtubule activity. Data from mice engrafted with the MDA-MB-231 triple-negative breast cancer cells showed that both CTR-17 and CTR-20 possess strong anticancer activity, alone or in combination with paclitaxel, without causing any notable side effects. Together, our data demonstrates that both the CTRs can be effective and safe drugs against many different cancers, especially against multidrug-resistant tumors.
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