Exploitation of new chalcones and 4H-chromenes as agents for cancer treatment

Pontes, Olívia; Costa, Marta; Santos, Filipa; Sampaio‐Marques, Belém; Dias, Tatiana A.; Ludovico, Paula; Baltazar, Fátima; Proença, M. Fernanda

doi:10.1016/j.ejmech.2018.07.058

Cited by 32 publications

(30 citation statements)

References 48 publications

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“…Propolis cytotoxicity was assessed by the sulforhodamine B (SRB) assay as previously described [47], which estimates cell biomass based on cell protein content. Briefly, each cell line was plated at an appropriate density (2000 cells/well for A498 and 786-O or 3000 cells/well for Caki-2 and HK2) in 96-well plates for 24 h. The dried extract and subfractions (by solvent evaporation) were dissolved in DMSO for the cells' treatments.…”

Section: Cytotoxicity Assay and Selectivity Index (Si) Calculationmentioning

confidence: 99%

Selective Cytotoxicity of Portuguese Propolis Ethyl Acetate Fraction towards Renal Cancer Cells

et al. 2022

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Renal cell carcinoma is the most lethal cancer of the urological system due to late diagnosis and treatment resistance. Propolis, a beehive product, is a valuable natural source of compounds with bioactivities and may be a beneficial addition to current anticancer treatments. A Portuguese propolis sample, its fractions (n-hexane, ethyl acetate, n-butanol and water) and three subfractions (P1–P3), were tested for their toxicity on A498, 786-O and Caki-2 renal cell carcinoma cell lines and the non-neoplastic HK2 kidney cells. The ethyl acetate fraction showed the strongest toxicity against A498 (IC50 = 0.162 µg mL−1) and 786-O (IC50 = 0.271 µg mL−1) cells. With similar toxicity against 786-O, P1 (IC50 = 3.8 µg mL−1) and P3 (IC50 = 3.1 µg mL−1) exhibited greater effect when combined (IC50 = 2.5 µg mL−1). Results support the potential of propolis and its constituents as promising coadjuvants in renal cell carcinoma treatment.

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Section: Cytotoxicity Assay and Selectivity Index (Si) Calculationmentioning

confidence: 99%

Selective Cytotoxicity of Portuguese Propolis Ethyl Acetate Fraction towards Renal Cancer Cells

et al. 2022

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“…Additionally, compound 14 exhibited an inhibitory effect against tubulin dynamics. Therefore, it may be a promising compound for inhibiting tubulin polymerization in the cancer cells (Pontes et al, 2018 ).…”

Section: Biological Activities Of 2h/4h-chromenesmentioning

confidence: 99%

2H/4H-Chromenes—A Versatile Biologically Attractive Scaffold

2020

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2H/4H-chromene (2H/4H-ch) is an important class of heterocyclic compounds with versatile biological profiles, a simple structure, and mild adverse effects. Researchers discovered several routes for the synthesis of a variety of 2H/4H-ch analogs that exhibited unusual activities by multiple mechanisms. The direct assessment of activities with the parent 2H/4H-ch derivative enables an orderly analysis of the structure-activity relationship (SAR) among the series. Additionally, 2H/4H-ch have numerous exciting biological activities, such as anticancer, anticonvulsant, antimicrobial, anticholinesterase, antituberculosis, and antidiabetic activities. This review is consequently an endeavor to highlight the diverse synthetic strategies, synthetic mechanism, various biological profiles, and SARs regarding the bioactive heterocycle, 2H/4H-ch. The presented scaffold work compiled in this article will be helpful to the scientific community for designing and developing potent leads of 2H/4H-ch analogs for their promising biological activities.

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“…Organic molecules containing quinoline or chromene moieties separately represent two important classes of heterocycles with noteworthy bio-activity. [1][2][3][4][5][6] Fused heterocycles are widely spread in nature and they often exhibit useful bio-activity. [7][8][9] Some fused naturally occurring quinoline alkaloids such as dictamnine, masculine,flindersiamine etc.…”

Section: Introductionmentioning

confidence: 99%

Recent Advances on Synthesis of Fused Chromeno‐Quinoline Heterocycles under Transition Metal‐Free Condition

Mal

Jana

2022

ChemistrySelect

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Among the various other organic compounds, the compounds having heterocyclic core are extensively circulated in nature and are often crucial for life. The concerned heterocyle may or may not be aromatic. They often show a variety of physiological, industrial and also theoretical significance. Quinoline derivatives are very popular anti-biotics and benzopyran or chromenes is another important heterocyclic moiety found widely in naturally occurring plant products like fruits and vegetables. However, when chromene and quinoline are present in a molecule in fused form, a subclass of very important bio-active chromene-fused quinoline heterocycles is formed. This review covers recent reports on transition metalfree synthesis of chromeno-quinoline derivatives in short and hassle-free reaction protocols.

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Exploitation of new chalcones and 4H-chromenes as agents for cancer treatment

Cited by 32 publications

References 48 publications

Selective Cytotoxicity of Portuguese Propolis Ethyl Acetate Fraction towards Renal Cancer Cells

Selective Cytotoxicity of Portuguese Propolis Ethyl Acetate Fraction towards Renal Cancer Cells

2H/4H-Chromenes—A Versatile Biologically Attractive Scaffold

Recent Advances on Synthesis of Fused Chromeno‐Quinoline Heterocycles under Transition Metal‐Free Condition

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