ArticleJournal of medicinal chemistry2013
Monocarbonyl curcumin analogues: heterocyclic pleiotropic kinase inhibitors that mediate anticancer properties.
Article in Journal of medicinal chemistry, 2013. 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, 35 citations in OpenAlex.
- Novel cyclic CCancer cell international · 2025Article
- Fluorinated andPharmaceutics · 2023Article
- Perspectives for synthetic curcumins in chemoprevention and treatment of cancer: An update with promising analogues.European journal of pharmacology · 2021Review
- Curcumin analog B14 has high bioavailability and enhances the effect of anti-breast cancer cells in vitro and in vivo.Cancer science · 2021Article
- Effects of green synthesised silver nanoparticles (ST06-AgNPs) using curcumin derivative (ST06) on human cervical cancer cells (HeLa) in vitro and EAC tumor bearing mice models.International journal of nanomedicine · 2019Article
- The Curcumin Analog CH-5 Exerts Anticancer Effects in Human Osteosarcoma Cells via Modulation of Transcription Factors p53/Sp1.International journal of molecular sciences · 2018Article
- Synthesis and Biological Evaluation of Curcumin Derivatives with Water-Soluble Groups as Potential Antitumor Agents: An in Vitro Investigation Using Tumor Cell Lines.Molecules (Basel, Switzerland) · 2015Article
- Monocarbonyl analogs of curcumin inhibit growth of antibiotic sensitive and resistant strains of Mycobacterium tuberculosis.European journal of medicinal chemistry · 2015Article
- Eliminating the heart from the curcumin molecule: monocarbonyl curcumin mimics (MACs).Molecules (Basel, Switzerland) · 2014Review
- Synthesis and evaluation of bisbenzylidenedioxotetrahydrothiopranones as activators of endoplasmic reticulum (ER) stress signaling pathways and apoptotic cell death in acute promyelocytic leukemic cells.Journal of medicinal chemistry · 2014Article
- Liver S9 Fraction-Derived Metabolites of Curcumin Analogue UBS109.ACS medicinal chemistry letters · 2014Article
- Design, synthesis, and evaluation of novel heteroaromatic analogs of curcumin as anti-cancer agents.European journal of medicinal chemistry · 2014Article
Corrections and comments
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Authors and funding
9 authors at 1 institution in 1 country.
Funding
Abstract
Curcumin is a biologically active component of curry powder. A structurally related class of mimetics possesses similar anti-inflammatory and anticancer properties. Mechanism has been examined by exploring kinase inhibition trends. In a screen of 50 kinases relevant to many forms of cancer, one member of the series (4, EF31) showed ≥85% inhibition for 10 of the enzymes at 5 μM, while 22 of the proteins were blocked at ≥40%. IC50 values for an expanded set of curcumin analogues established a rank order of potencies, and analyses of IKKβ and AKT2 enzyme kinetics for 4 revealed a mixed inhibition model, ATP competition dominating. Our curcumin mimetics are generally selective for Ser/Thr kinases. Both selectivity and potency trends are compatible with protein sequence comparisons, while modeled kinase binding site geometries deliver a reasonable correlation with mixed inhibition. Overall, these analogues are shown to be pleiotropic inhibitors that operate at multiple points along cell signaling pathways.
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Registered trials
Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.