ArticleInvestigational new drugs2011
Mechanisms for the activity of heterocyclic cyclohexanone curcumin derivatives in estrogen receptor negative human breast cancer cell lines.
Article in Investigational new drugs, 2011. 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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Who cites it
25 citing papers in PubMed, 77 citations in OpenAlex.
- Natural anti-cancer products: insights from herbal medicine.Chinese medicine · 2025Review
- Synthetic Curcumin Analogs in the Treatment of Cancer: A Literature Review.Current medicinal chemistry · 2025Review
- Therapeutic potential of curcumin and its nanoformulations for treating oral cancer.World journal of methodology · 2023Review
- Bioactive compounds, antibacterial and antioxidant activities of methanol extract of Tamarindus indica Linn.Scientific reports · 2022Article
- Raloxifene Suppresses Tumor Growth and Metastasis in an Orthotopic Model of Castration-Resistant Prostate Cancer.Biomedicines · 2022Article
- Potential Role of Curcumin and Its Nanoformulations to Treat Various Types of Cancers.Biomolecules · 2021Review
- Curcumin analog B14 has high bioavailability and enhances the effect of anti-breast cancer cells in vitro and in vivo.Cancer science · 2021Article
- Dienone Compounds: Targets and Pharmacological Responses.Journal of medicinal chemistry · 2020Article
- Therapeutic role of curcumin and its novel formulations in gynecological cancers.Journal of ovarian research · 2020Review
- Curcumin and Its Derivatives as Potential Therapeutic Agents in Prostate, Colon and Breast Cancers.Molecules (Basel, Switzerland) · 2019Review
- A multivariate statistical analysis of the effects of styrene maleic acid encapsulated RL71 in a xenograft model of triple negative breast cancer.Journal of biological methods · 2019Article
- Design, synthesis and cytotoxic effects of curcuminoids on HeLa, K562, MCF-7 and MDA-MB-231 cancer cell lines.Chemistry Central journal · 2018Article
- The aryl hydrocarbon receptor as an antitumor target of synthetic curcuminoids in colorectal cancer.The Journal of surgical research · 2017Article
- Bringing Curcumin to the Clinic in Cancer Prevention: a Review of Strategies to Enhance Bioavailability and Efficacy.The AAPS journal · 2017Review
- Styrene maleic acid-encapsulated RL71 micelles suppress tumor growth in a murine xenograft model of triple negative breast cancer.International journal of nanomedicine · 2017Article
- A combination of sorafenib and nilotinib reduces the growth of castrate-resistant prostate cancer.International journal of nanomedicine · 2016Article
- Combination of α-Tomatine and Curcumin Inhibits Growth and Induces Apoptosis in Human Prostate Cancer Cells.PloS one · 2015Article
- A novel role for raloxifene nanomicelles in management of castrate resistant prostate cancer.BioMed research international · 2014Article
- Curcumin: a potential candidate in prevention of cancer via modulation of molecular pathways.BioMed research international · 2014Review
- Perspectives on new synthetic curcumin analogs and their potential anticancer properties.Current pharmaceutical design · 2013Review
Corrections and comments
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Authors and funding
6 authors at 3 institutions in 2 countries.
Funding
No grant is acknowledged in the PubMed record.
Abstract
Estrogen receptor (ER)-negative breast cancer is an aggressive form that currently requires more drug treatment options. Thus, we have further modified cyclohexanone derivatives of curcumin and examined them for cytotoxicity towards ER-negative human breast cancer cells. Two of the analogs screened elicited increased cytotoxic potency compared to curcumin and other previously studied derivatives. Specifically, 2,6-bis(pyridin-3-ylmethylene)-cyclohexanone (RL90) and 2,6-bis(pyridin-4-ylmethylene)-cyclohexanone (RL91) elicited EC(50) values of 1.54 and 1.10 µM, respectively, in MDA-MB-231 cells and EC(50) values of 0.51 and 0.23 in SKBr3 cells. All other new compounds examined were less potent than curcumin, which elicited EC(50) values of 7.6 and 2.4 µM in MDA-MB-231 and SKBr3 cells, respectively. Mechanistic analyses demonstrated that RL90 and RL91 significantly induced G(2)/M-phase cell cycle arrest and apoptosis. RL90 and RL91 also modulated the expression of key cell signaling proteins, specifically, in SKBr3 cells, protein levels of Her-2, Akt, and NFκB were decreased in a time-dependent manner, while activity of stress kinases JNK1/2 and P38 MAPK were increased. Signaling events in MDA-MB-231 cells were differently implicated, as EGFR protein levels were decreased and activity of GSK-3β transiently decreased, while β-catenin protein level and activity of P38 MAPK, Akt, and JNK1/2 were transiently increased. In conclusion replacement of the phenyl group of cyclohexanone derived curcumin derivatives with heterocyclic rings forms a class of second-generation analogs that are more potent than both curcumin and other derivatives. These new derivatives provide a platform for the further development of drugs for the treatment of ER-negative breast cancer.
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