ArticleCancer chemotherapy and pharmacology2014
Mouse pharmacokinetics and metabolism of the curcumin analog, 4-piperidinone,3,5-bis[(2-fluorophenyl)methylene]-acetate(3E,5E) (EF-24; NSC 716993).
Article in Cancer chemotherapy and pharmacology, 2014. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 26 papers.
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Who cites it
26 citing papers in PubMed.
- In Vitro and In Silico Evaluation of the Anti-Infective Potential of EF24-Analogous Curcuminoids: Antiprotozoal Activity and HIV-1 Ribonuclease H Inhibition.Pathogens (Basel, Switzerland) · 2026Article
- mCellular and molecular life sciences : CMLS · 2025Article
- Synthesis, Anti-Tumour, and Antibacterial Activities of Monocarbonyl Curcumin Analogues of Piperidones.International journal of molecular sciences · 2025Article
- EF24 targets METTL3 to reprogram m6A methylation and induce ferroptosis: an epitranscriptomic mechanism with therapeutical potential for glioma.Cell communication and signaling : CCS · 2025Article
- Curcumin and acute myeloid leukemia: a golden hope, updated insights.Molecular biology reports · 2025Review
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- Review
- Therapeutic potential of curcumin and its nanoformulations for treating oral cancer.World journal of methodology · 2023Review
- The Curcuminoid EF24 in Combination with TRAIL Reduces Human Renal Cancer Cell Migration by Decreasing MMP-2/MMP-9 Activity through a Reduction in HInternational journal of molecular sciences · 2023Article
- Curcumin and its Analogs and Carriers: Potential Therapeutic Strategies for Human Osteosarcoma.International journal of biological sciences · 2023Review
- FLLL32 Triggers Caspase-Mediated Apoptotic Cell Death in Human Oral Cancer Cells by Regulating the p38 Pathway.International journal of molecular sciences · 2021Article
- Effects of Curcumin Analogues DMC and EF24 in Combination with the Cytokine TRAIL against Kidney Cancer.Molecules (Basel, Switzerland) · 2021Article
- Antitumoral Activities of Curcumin and Recent Advances to ImProve Its Oral Bioavailability.Biomedicines · 2021Review
- Perspectives for synthetic curcumins in chemoprevention and treatment of cancer: An update with promising analogues.European journal of pharmacology · 2021Review
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- Article
- Inhibition of breast cancer metastasis to the lungs with UBS109.Oncotarget · 2018Article
- Bioactivities of EF24, a Novel Curcumin Analog: A Review.Frontiers in oncology · 2018Review
- Enhancement of Curcumin Bioavailability Via the Prodrug Approach: Challenges and Prospects.European journal of drug metabolism and pharmacokinetics · 2017Review
- FM807, a curcumin analogue, shows potent antitumor effects in nasopharyngeal carcinoma cells by heat shock protein 90 inhibition.Oncotarget · 2017Article
Corrections and comments
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Authors and funding
7 authors.
Funding
Abstract
purposeCurcumin, a keto-enol constituent of turmeric, has in vitro and in vivo antitumor activity. However, in vivo potency is low due to poor oral absorption. The mono-carbonyl analog, 3,5-bis[(2-fluorophenyl)methylene]-4-piperidinone acetate (EF-24, NSC 716993), exhibited broad-spectrum activity in the NCI anticancer cell line screen and potent antiangiogenesis activity in a HUVEC cell migration assay. The purpose of this study was to characterize the preclinical pharmacology of EF-24 in mice.
methodsEF-24 plasma stability, protein binding, pharmacokinetics, and metabolism were characterized utilizing an LC/MS/MS assay.
resultsAn LC/MS/MS assay incorporated protein precipitation with methanol, reverse-phase HPLC separation under gradient elution using an aqueous methanol mobile phase containing 0.1 % formic acid, and positive electrospray ionization detection of the m/z 312 > 149 transition for EF-24. The assay was linear over the range 7.8-1,000 nM. Plasma protein binding was >98 % with preferential binding to albumin. EF-24 plasma disposition in mice after i.v. administration of a 10 mg/kg dose was best fit to a 3-compartment open model. The terminal elimination half-life and plasma clearance values were 73.6 min and 0.482 L/min/kg, respectively. EF-24 bioavailability was 60 and 35 % after oral and i.p. administration, respectively. NADPH-dependent metabolism of EF-24 loss in liver microsomal preparations yielded several metabolites consistent with EF-24 hydroxylation and reduction.
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