ArticleBioorganic & medicinal chemistry2021
Synthesis and structure-activity relationship of coumarins as potent Mcl-1 inhibitors for cancer treatment.
Article in Bioorganic & medicinal chemistry, 2021. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 5 papers.
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Who cites it
5 citing papers in PubMed, 29 citations in OpenAlex.
- Evaluation ofFood science & nutrition · 2025Article
- Application of the Mannich reaction in the structural modification of natural products.Journal of enzyme inhibition and medicinal chemistry · 2023Review
- Synthesis and Biological Evaluation of Coumarin Triazoles as Dual Inhibitors of Cholinesterases and β-Secretase.ACS omega · 2023Article
- Synthesis and biological evaluation of esculetin derivatives as potential anti-HBV agents.Medicinal chemistry research : an international journal for rapid communications on design and mechanisms of action of biologically active agents · 2023Article
- Optical substrates for drug-metabolizing enzymes: Recent advances and future perspectives.Acta pharmaceutica Sinica. B · 2022Review
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Authors and funding
7 authors at 5 institutions in 2 countries.
Funding
Abstract
Myeloid cell leukemia-1 (Mcl-1) is a validated and attractive target for cancer therapy. Over-expression of Mcl-1 in many cancers allows cancer cells to evade apoptosis and contributes to their resistance to current chemotherapeutics. In this study, more than thirty coumarin derivatives with different substituents were designed and synthesized, and their Mcl-1 inhibitory activities evaluated using a fluorescence polarization-based binding assay. The results showed that the catechol group was a key constituent for Mcl-1 inhibitory activity of the coumarins, and methylation of the catechol group led to decreased inhibitory activity. The introduction of a hydrophobic electron-withdrawing group at the C-4 position of 6,7-dihydroxycoumarin, enhanced Mcl-1 inhibitory capacity, and a hydrophilic group in this position was unbeneficial to the inhibitory potency. In addition, the introduction of a nitrogen-containing group to the C-5 or C-8 position, which allowed an intramolecular hydrogen bond, was also unfavorable for Mcl-1 inhibition. Among all coumarins tested, 4-trifluoromethyl-6,7-dihydroxycoumarin (Cpd 4) displayed the most potent inhibitory activity towards Mcl-1 (K
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