A High-throughput Screening of a Chemical Compound Library in Ovarian Cancer Stem Cells

Ricci, Francesca; Carrassa, Laura; Christodoulou, Michael S.; Passarella, Daniele; Michel, Benoît Y.; Benhida, Rachid; Martinet, Nadine; Hunyadi, Attila; Iοannou, Efstathia; Roussis, Vassilios; Musso, Loana; Dallavalle, Sabrina; Silvestri, Romano; Westwood, Nicholas J.; Mori, Mattia; Ingallina, Cinzia; Botta, Bruno; Kavetsou, Eleni; Detsi, Anastasia; Májer, Zsuzsa; Hudecz, Ferenc; Bősze, Szilvia; Kamińska, Bożena; Hansen, Trond Vidar; Bertrand, Philìppe; Athanassopoulos, Constantinos M.; Damia, Giovanna

doi:10.2174/1386207321666180124093406

Cited by 3 publications

(3 citation statements)

References 31 publications

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“…Coumarins are naturally plant‐derived or synthetically obtained substances that belong to the benzopyrone family (Detsi, Kontogiorgis, & Hadjipavlou‐Litina, ). The wide bioactivity array, such as antioxidant (Matos et al, ), anti‐inflammatory (Melagraki et al, ; Roussaki et al, ), anticancer (Kavetsou et al, ; Ricci et al, ), antivirus (Atta‐ur‐Rahman., ), and neuroprotective (Okuyama et al, ), renders coumarins attractive for further evaluation as novel therapeutic agents. Research has shown that substitution on the coumarin scaffold strongly influences its pharmacological profile.…”

Section: Introductionmentioning

confidence: 99%

Novel 3‐aryl‐5‐substituted‐coumarin analogues: Synthesis and bioactivity profile

Kavetsou

Katopodi

Argyri

et al. 2020

Drug Development Research

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Eighteen 3-aryl-5-substituted-coumarins-six 5-acetyloxy-derivatives, six 5-hydroxyderivatives, and six 5-geranyloxy-derivatives-were synthesized, structurally characterized and their antioxidant activity, lipoxygenase inhibitory ability, as well as their cytotoxic activity against human neuroblastoma SK-N-SH and HeLa adenocarcinoma cell lines were evaluated. The 5-acetyloxy-compounds 3a-3f were found to be the best cytotoxic agents among all the compounds studied. The bromo-substituted coumarins 3a and 3b were remarkably active against HeLa cell line showing IC 50 1.8 and 6.1 μM, respectively. Coumarin 5e possessing a geranyloxy-chain on position 5 of the coumarin scaffold presented dual bioactivity, while 5-geranyloxy-coumarin 5f was the most competent soybean lipoxygenase inhibitor of this series (IC 50 10 μM). As shown by in silico docking studies, the studied molecules present allosteric interactions with soybean lipoxygenases.

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Section: Introductionmentioning

confidence: 99%

Novel 3‐aryl‐5‐substituted‐coumarin analogues: Synthesis and bioactivity profile

Kavetsou

Katopodi

Argyri

et al. 2020

Drug Development Research

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“…Coumarin derivatives have gained high scientific interest as promising drug candidates since they possess multiple pharmacological properties [10][11][12][13], such as antioxidant [14][15][16], antibacterial [17,18], antimicrobial [18], antiviral [13], hepatoprotective [19] and anti-inflammatory effects [20][21][22]. Natural and synthetic coumarins have been also reported as effective chemopreventive and anticancer agents in vitro [23][24][25][26] and in vivo [27].…”

Section: Introductionmentioning

confidence: 99%

Investigation of the cytotoxicity of bioinspired coumarin analogues towards human breast cancer cells

et al. 2020

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Coumarins possess a wide array of therapeutic capabilities, but often with unclear mechanism of action. We tested a small library of 18 coumarin derivatives against human invasive breast ductal carcinoma cells with the capacity of each compound to inhibit cell proliferation scored, and the most potent coumarin analogues selected for further studies. Interestingly, the presence of two prenyloxy groups (5,7-diprenyloxy-4-methyl-coumarin, 4g) or the presence of octyloxy substituent (coumarin 4d) was found to increase the potency of compounds in breast cancer cells, but not against healthy human fibroblasts. The activity of potent compounds on breast cancer cells cultured more similarly to the conditions of the tumour microenvironment was also investigated, and increased toxicity was observed. Results suggest that tested coumarin derivatives could potentially reduce the growth of tumour mass. Moreover, their use as (combination) therapy in cancer treatment might have the potential of causing limited side effects. Leonidas Gkionis and Eleni Kavetsou: Co-first authors.

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“…Peptide-based drugs could also be screened from natural environment, such as terrestrial and marine environments [516]. The development of high throughput screening method, i.e., phage display and one-bead-one-compound, contributed to the screening of peptide-based drugs for cancer therapy [517]. Peptide would activate or antagonize the protein and related signaling pathways, such as inhibiting the secret of testosterone, achieving the anti-cancer effects.…”

Section: Peptide Monomer For Cancer Therapymentioning

confidence: 99%

Biomedical polymers: synthesis, properties, and applications

Chen

et al. 2022

Sci. China Chem.

117

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Biomedical polymers have been extensively developed for promising applications in a lot of biomedical fields, such as therapeutic medicine delivery, disease detection and diagnosis, biosensing, regenerative medicine, and disease treatment. In this review, we summarize the most recent advances in the synthesis and application of biomedical polymers, and discuss the comprehensive understanding of their property-function relationship for corresponding biomedical applications. In particular, a few burgeoning bioactive polymers, such as peptide/biomembrane/microorganism/cell-based biomedical polymers, are also introduced and highlighted as the emerging biomaterials for cancer precision therapy. Furthermore, the foreseeable challenges and outlook of the development of more efficient, healthier and safer biomedical polymers are discussed. We wish this systemic and comprehensive review on highlighting frontier progress of biomedical polymers could inspire and promote new breakthrough in fundamental research and clinical translation.

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A High-throughput Screening of a Chemical Compound Library in Ovarian Cancer Stem Cells

Cited by 3 publications

References 31 publications

Novel 3‐aryl‐5‐substituted‐coumarin analogues: Synthesis and bioactivity profile

Novel 3‐aryl‐5‐substituted‐coumarin analogues: Synthesis and bioactivity profile

Investigation of the cytotoxicity of bioinspired coumarin analogues towards human breast cancer cells

Biomedical polymers: synthesis, properties, and applications

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