Synthesis of New Cyanopyridine Scaffolds and their Biological Activities

2020 ◽  
Vol 17 (7) ◽  
pp. 567-575
Author(s):  
Nabil A. Alhakamy ◽  
Ahmad O. Noor ◽  
Khaled M. Hosny ◽  
Jenny Jeehan Nasr ◽  
Moustafa M.G. Fouda ◽  
...  
Keyword(s):  
Vitamin C ◽  
Cytotoxic Activity ◽  
Cell Lines ◽  
Biological Activities ◽  
Biological Effects ◽  
Tuberculosis H37rv ◽  
Cytotoxic Agents ◽  
H37rv Strain ◽  
Dpph Method

Background: 3-Cyanopyridine analogues are significant moieties with a variety of biological effects such as antioxidant, antimicrobial, anti-inflammatory and cytotoxic agents. In addition, they could be applied in the treatment of several diseases. Objective: The study conducted cyclo-addition of 3a-e derivatives with malononitrile to yield the corresponding 6-(4-((3-cyano-pyridinyl) amino) phenyl)-4-phenylnicotinonitriles 4a-e. Materials and Methods: Physical and spectral analyses were performed to demonstrate the proper structures of all incorporated analogues. The in vitro antimicrobial activity of the preps derivatives was investigated by testing them with a panel of pathogenic strains of bacteria and fungi. The anti-tuberculosis activity was observed against the Mycobacterium tuberculosis H37Rv strain. When examining cytotoxic agents for four different cell lines, researchers found that their activity was persuasive compared with that of standard antibiotics. In addition, the antioxidant activity of the synthesized analogues was evaluated using the DPPH method. Results and Discussions: The synthesized analogues were examined to determine their activity against the M. tuberculosis H37Rv strain. Derivatives 2c, 2e, 3d and 3e had good inhibition. Further screening was done for the highest potency against M. tuberculosis to determine the MICs. The antioxidant efficacy was evaluated via the DPPH technique matched with vitamin C as a positive control. The prospective results showed that the derivatives did not display scavenging efficacies in comparison with the standard. Conclusion: Some synthesized derivatives displayed good potency against bacterial activity and M. Tuberculosis. However, the antioxidant performance of these derivatives did not display scavenging efficacies compared to vitamin C. The cytotoxic activity of the synthesized derivatives was examined against various cell lines to display good cytotoxic activity in the order 4a-e > 2a-e > 3a-b.

scholarly journals Biological Effects of Glucosinolate Degradation Products from Horseradish: A Horse that Wins the Race

Biomolecules ◽  
2020 ◽  
Vol 10 (2) ◽  
pp. 343 ◽  
Author(s):  
Marijana Popović ◽  
Ana Maravić ◽  
Vedrana Čikeš Čulić ◽  
Azra Đulović ◽  
Franko Burčul ◽  
...  
Keyword(s):  
Cytotoxic Activity ◽  
Cell Lines ◽  
Cancer Cell ◽  
Degradation Products ◽  
Human Cancer ◽  
Biological Activities ◽  
Biological Effects ◽  
Cancer Cell Lines ◽  
Cytotoxic Activities ◽  
Minimal Inhibitory Concentrations

Horseradish degradation products, mainly isothiocyanates (ITC) and nitriles, along with their precursors glucosinolates, were characterized by GC-MS and UHPLC-MS/MS, respectively. Volatiles from horseradish leaves and roots were isolated using microwave assisted-distillation (MAD), microwave hydrodiffusion and gravity (MHG) and hydrodistillation (HD). Allyl ITC was predominant in the leaves regardless of the isolation method while MAD, MHG, and HD of the roots resulted in different yields of allyl ITC, 2-phenylethyl ITC, and their nitriles. The antimicrobial potential of roots volatiles and their main compounds was assessed against sixteen emerging food spoilage and opportunistic pathogens. The MHG isolate was the most active, inhibiting bacteria at minimal inhibitory concentrations (MICs) from only 3.75 to 30 µg/mL, and fungi at MIC50 between <0.12 and 0.47 µg/mL. Cytotoxic activity of volatile isolates and their main compounds were tested against two human cancer cell lines using MTT assay after 72 h. The roots volatiles showed best cytotoxic activity (HD; IC50 = 2.62 μg/mL) against human lung A549 and human bladder T24 cancer cell lines (HD; IC50 = 0.57 μg/mL). Generally, 2-phenylethyl ITC, which was tested for its antimicrobial and cytotoxic activities along with two other major components allyl ITC and 3-phenylpropanenitrile, showed the best biological activities.

scholarly journals UPLC-ESI-MS/MS Profile and Antioxidant, Cytotoxic, Antidiabetic, and Antiobesity Activities of the Aqueous Extracts of Three Different Hibiscus Species

2020 ◽  
Vol 2020 ◽  
pp. 1-17
Author(s):  
Hanan M. Al-Yousef ◽  
Wafaa H. B. Hassan ◽  
Sahar Abdelaziz ◽  
Musarat Amina ◽  
Rasha Adel ◽  
...  
Keyword(s):  
Cytotoxic Activity ◽  
Aqueous Extract ◽  
Biological Activities ◽  
Biological Effects ◽  
Aqueous Extracts ◽  
Potent Effect ◽  
Esi Ms ◽  
Biological Studies ◽  
Hct 116

The aqueous extracts of Hibiscus calyphyllus (HcA), Hibiscus micranthus (HmA), and Hibiscus deflersii (HdA) growing in Saudi Arabia did not receive enough attention in phytochemical and biological studies. This inspired the authors to investigate the phytochemicals of these extracts for the first time using UPLC-ESI-MS/MS in negative and positive ionization modes. The analysis afforded the tentative identification of 103 compounds including phenolic compounds, flavonoids, and anthocyanins. Moreover, in vitro evaluations of their cytotoxic, antioxidant, antidiabetic, and antiobesity activities were carried out. The results showed that aqueous extract of Hibiscus calyphyllus had the highest activity as an antioxidant agent (SC50 = 111 ± 1.5 μg/mL) compared with ascorbic acid (SC50 = 14.2 ± 0.5 μg/mL). MTT assay was used to evaluate cytotoxic activity compared to cisplatin. Hibiscus deflersii showed the most potent cytotoxic effect against A-549 (human lung carcinoma) with IC50 = 50 ± 5.1 μg/mL, and Hibiscus micranthus showed a close effect with IC50 = 60.4 ± 1.7 μg/mL. Hibiscus micranthus showed the most potent effect on HCT-116 (human colon carcinoma) with IC50 = 56 ± 1.9 μg/mL compared with cisplatin (IC50 = 7.53 ± 3.8 μg/mL). HcA and HdA extracts showed weak cytotoxic activity against A-549 and HCT-116 cell lines compared to the other extracts. Eventually, Hibiscus deflersii showed astonishing antidiabetic (IC50 = 56 ± 1.9 μg/mL) and antiobesity (IC50 = 95.45 ± 1.9 μg/mL) activities using in vitro α-amylase inhibitory assay (compared with acarbose (IC50 = 34.71 ± 0.7 μg/mL)) and pancreatic lipase inhibitory assay (compared with orlistat (IC50 = 23.8 ± 0.7 μg/mL)), respectively. In conclusion, these findings are regarded as the first vision of the phytochemical constituents and biological activities of different Hibiscus aqueous extracts. Hibiscus deflersii aqueous extract might be a hopeful origin of functional constituents with anticancer (on A-549 cell line), antidiabetic, and antiobesity activities. It might be a natural alternative remedy and nutritional policy for diabetes and obesity treatment without negative side effects. Isolation of the bioactive phytochemicals from the aqueous extracts of aerial parts of Hibiscus calyphyllus, Hibiscus micranthus, and Hibiscus deflersii and estimation of their biological effects are recommended in further studies.

Design, Synthesis and Antiproliferative Evaluation of Novel 1,2,4-Triazole/Schiff Base Hybrids with EGFR and B-RAF Inhibitory Activities

2019 ◽  
Vol 19 (5) ◽  
pp. 697-706 ◽  
Author(s):  
Hany A.M. El-Sherief ◽  
Bahaa G.M. Youssif ◽  
Ahmed H. Abdelazeem ◽  
Mohamed Abdel-Aziz ◽  
Hamdy M. Abdel-Rahman
Keyword(s):  
Cancer Cells ◽  
Cell Lines ◽  
Cancer Cell ◽  
Antiproliferative Activity ◽  
Human Cancer ◽  
Biological Activities ◽  
Cytotoxic Agents ◽  
Human Pancreas ◽  
Screening Assay

Background: 1,2,4-triazoles possess a broad spectrum of biological activities such as analgesic, antimicrobial, antitubercular, anti-inflammatory and antineoplastic activities. This heterocycle and their derivatives were included into a wide variety of therapeutically interesting drugs. Hence, it is of great interest to explore new 1,2,4-triazoles as cytotoxic agents targeting EGFR, B-Raf kinases. Methods: The final compounds 9a-b, 10a-b, 11a-b, 12a-b, 13a-b and 14a-f were prepared by refluxing a mixture of triazole 3a-b and 7a-d with the corresponding benzaldehyde derivatives 8a-d in absolute ethanol to afford the target final compounds in good yields. The newly synthesized triazole-containing compounds were assessed according to standard protocols for their in vitro antiproliferative activity against four human cancer cell lines including human pancreas cancer cell line (Panc-1), pancreatic carcinoma cells (PaCa-2), colon cancer cells (HT-29) and lung cancer cells (H-460) using the propidium iodide (PI) fluorescence assay. Compounds 9a and 13a were evaluated against EGFR, B-Raf and Tubulin anticancer targets. Results: Compounds 9a, 9b, 10a, 11a, 12a, 13a and 13b showed remarkable antiproliferative activity against the tested cell lines with IC50 range of 1.3-5.9µM. Compounds 9a and 13a with the least IC50 values in the anticancer screening assay were tested against three known anticancer targets including EGFR, B-Raf kinase and Tubulin. The results revealed that compound 13a showed the highest potency against B-Raf and EGFR kinases with IC50 = 0.7 and 1.9 µM, respectively. Conclusion: 1,2,4-triazoles reported herein are potent EGFR, B-Raf inhibitors. These lead compounds will be subjected to more detailed mechanistic studies.

scholarly journals Walnut (Juglans regia L.) Septum: Assessment of Bioactive Molecules and In Vitro Biological Effects

Molecules ◽  
2020 ◽  
Vol 25 (9) ◽  
pp. 2187
Author(s):  
Marius Emil Rusu ◽  
Ionel Fizesan ◽  
Anca Pop ◽  
Andrei Mocan ◽  
Ana-Maria Gheldiu ◽  
...  
Keyword(s):  
Cell Lines ◽  
Salmonella Enteritidis ◽  
Biological Activities ◽  
Biological Effects ◽  
Juglans Regia ◽  
Interleukin 1 ◽  
Bioactive Compound ◽  
Cell Types ◽  
Bioactive Molecules

Walnut (Juglans regia L.) septum represents an interesting bioactive compound source by-product. In our study, a rich phenolic walnut septum extract, previously selected, was further examined. The tocopherol content determined by liquid chromatography-tandem mass spectrometry (LC-MS/MS) revealed higher amounts of α-tocopherol compared to γ- and δ-tocopherols. Moreover, several biological activities were investigated. The in vitro inhibiting assessment against acetylcholinesterase, α-glucosidase, or lipase attested a real management potential in diabetes or obesity. The extract demonstrated very strong antimicrobial potential against Staphylococcus aureus, Pseudomonas aeruginosa and Salmonella enteritidis. It also revealed moderate (36.08%) and strong (43.27%) antimutagenic inhibitory effects against TA 98 and TA 100 strains. The cytotoxicity of the extract was assessed on cancerous (A549, T47D-KBluc, MCF-7) and normal (human gingival fibroblasts (HGF)) cell lines. Flow cytometry measurements confirmed the cytotoxicity of the extract in the cancerous cell lines. Additionally, the extract demonstrated antioxidant activity on all four cell types, as well as anti-inflammatory activity by lowering the inflammatory cytokines (interleukin-6 (IL-6), interleukin-8 (IL-8), interleukin-1 β (IL-1β)) evaluated in HGF cells. To the best of our knowledge, most of the cellular model analyses were performed for the first time in this matrix. The results prove that walnut septum may be a potential phytochemical source for pharmaceutical and food industry.

SYNTHESIS, CYTOTOXIC EVALUATION AND MOLECULAR DOCKING STUDIES OF NEW 3-(1,3,4-OXADIAZOLYL)-QUINOLINONE DERIVATIVES AGAINST BREAST CANCER CELL LINES

INDIAN DRUGS ◽  
2018 ◽  
Vol 55 (11) ◽  
pp. 19-31
Author(s):  
S Muthadi ◽  
◽  
R. Guda ◽  
M. Kasula ◽  
A Garlapati ◽  
...  
Keyword(s):  
Breast Cancer ◽  
Cytotoxic Activity ◽  
Cell Lines ◽  
Cancer Cell ◽  
Breast Cancer Cell ◽  
Cancer Cell Lines ◽  
Docking Studies ◽  
Breast Cancer Cell Lines ◽  
Dpph Method

A series of new substituted 3-(5-substituted-1,3,4-oxadiazol-2-yl)-4(1H)-quinolinone derivatives (5a-t) have been designed and synthesized using appropriate protocols. All of them were screened for cytotoxic activity against human breast cancer cell lines (MCF-7 and T47D) and antioxidant activity (DPPH method). Among them, 5f exhibited promising inhibitory activity with IC50 values 7.429 and 8.388 against the two cell lines chosen. The molecular interactions with target (aromatase receptor by docking) were found to correlate well with in vitro cytotoxic activity, i.e. 5f showed the high binding affinity -12.34 kcal/ mol. In the antioxidant screening also, 5f and 5h were found superior to others.

Development of New IDO Inhibitors with Coumarin Pyrimidine Scaffolds as the Potential Anti Cancer Agents

2020 ◽  
Vol 16 (8) ◽  
pp. 1172-1180
Author(s):  
Radhika Chelamalla ◽  
Ajitha Makula
Keyword(s):  
Cytotoxic Activity ◽  
Cell Lines ◽  
Mtt Assay ◽  
Human Cancer ◽  
Docking Studies ◽  
Cytotoxic Agents ◽  
Ongoing Research ◽  
Human Cancer Cell Lines ◽  
Ic50 Values

Background: Progress in the developments of pyrimidine-coumarin moiety as an IDO inhibitor is still continuing with an outcome of the good scaffold as pyrimidine as well as coumarin individually for anticancer activity. Hence we proposed a suitable approach for the synthesis of pyrimidinecoumarin moieties in a combined form from the results of docking studies. Objective: As part of our ongoing research towards the development of novel cytotoxic agents, the synthesis and cytotoxic activity of a series of N'-(1-(6-methyl-2-oxo/thioxo-4-sub phenyl-1,2,3,4- tetrahydropyrimidin-5-yl)vinyl)-2-oxo-2H-chromene-3-carbohydrazide derivatives are discussed in this study. Methods: N'-(1-(6-methyl-2-oxo/thioxo-4-sub phenyl-1,2,3,4-tetrahydropyrimidin-5-yl)vinyl)-2-oxo- 2H-chromene-3-carbohydrazide derivatives were designed, synthesized and evaluated for cytotoxic activity. The structures were confirmed by IR, 1H NMR, C13NMR, Mass spectroscopy. All the synthesized compounds were evaluated using in vitro MTT assay against HeLa and HepG2 cell lines. Results: Compound 6g showed inhibitory activity against IDO with IC50 values at nanomolar range in docking studies and compounds 6g and 6f also showed significant cytotoxic activity on human cancer cell lines like HepG2 and HeLa using in vitro MTT assay. Conclusion: This work showed that the coumarin containing pyrimidine derivatives are found to be the most potent against IDO through docking studies and cytotoxic against cell lines compared with cisplatin. This might give the information for the development of new series of compounds against IDO.

Synthesis and Antimicrobial Activity of Adamantyl Substituted Pyridoxine Derivatives

2019 ◽  
Vol 16 (12) ◽  
pp. 1360-1369 ◽  
Author(s):  
Rail Khaziev ◽  
Nikita Shtyrlin ◽  
Roman Pavelyev ◽  
Raushan Nigmatullin ◽  
Raylya Gabbasova ◽  
...  
Keyword(s):  
Influenza Virus ◽  
Lipid Membranes ◽  
Specific Activity ◽  
Tuberculosis H37rv ◽  
Microbial Pathogens ◽  
Adamantane Derivatives ◽  
Carbon Cage ◽  
H37rv Strain ◽  
Derivatives Of

Background: Adamantane derivatives possess multiple pharmacological activities such as antiviral, anticancer, antimycobacterial, antidiabetic, antiparkinsonian and others. The interest of medicinal chemists in adamantane compounds is due to their unique spatial structure, high lipophilicity, and carbon cage rigidity. As a result, these molecules can easily penetrate biological lipid membranes and often have unique target-specific activity profile. Another pharmacophore studied in this work is pyridoxine (vitamin B6). Pyridoxine plays highly important roles in living cells as a key cofactor of many enzymes. On the other hand, its molecular scaffold is a valuable structural platform which has led to the development of several launched drugs (Pyritinol, Pirisudanol, Cycletanine, Mangafodipir) and a wide number of preclinical and clinical drug candidates. Objective: The objective of this study is a synthesis of pyridoxine-adamantane and pyridoxinecyclooctane dipharmacophore molecules. The underlying idea was to assess the antibacterial and antiviral potential of such dipharmacophores, based on multiple examples of promising antiinfective agents which have in their structures adamantane and pyridoxine moieties. Another specific reason was to explore the ability of pyridoxine pharmacophore to suppress the potential of microbial pathogens to develop resistance to drug molecules. Methods: In this study, a series of pyridoxine-adamantane and pyridoxine-cyclooctane dipharmacophore molecules were synthesized based on reactions of three different cycloalkyl amines with the corresponding electrophilic derivatives of pyridoxine aldehydes, chlorides and acetates. All synthesized compounds have been tested for their in vitro activity against M. tuberculosis H37Rv strain and H3N2 (A/Aichi/2/68) influenza virus. Results: Series of pyridoxine-adamantane and pyridoxine-cyclooctane dipharmacophore molecules were synthesized based on reactions of three different cycloalkylamines with the corresponding electrophilic derivatives of pyridoxine aldehydes, chlorides and acetates. Reaction of cycloalkylamines with pyridoxine derivatives, in which meta-hydroxyl and ortho-hydroxymethyl groups are protected by acetyl groups, represents a useful alternative to reductive amination of aldehydes and nucleophilic substitution of alkyl halides. According to a tentative mechanism, it proceeds via paraand ortho-pyridinone methides which readily react with nucleophiles. None of the synthesized dipharmacophore compounds showed activity against M. tuberculosis H37Rv strain. At the same time, three compounds demonstrated some antiviral activity against H3N2 (A/Aichi/2/68) influenza virus (EC50 52-88 µg/mL) that was comparable to the activity of Amantadine, though lower than the activity of Rimantadine. The results of this work can be useful in the design of physiologically active derivatives of pyridoxine and adamantane. Conclusion: The results of this work can be useful in the design of physiologically active derivatives of pyridoxine and adamantane.

1'-methylspiro[indoline-3,4'-piperidine] Derivatives: Design, Synthesis, Molecular Docking and Anti-tumor Activity Studies

2020 ◽  
Vol 17 ◽  
Author(s):  
Junjian Li ◽  
Lianbao Ye ◽  
Yuanyuan Wang ◽  
Ying Liu ◽  
Xiaobao Jin ◽  
...  
Keyword(s):  
Molecular Docking ◽  
Cell Lines ◽  
Active Sites ◽  
Biological Activities ◽  
Significant Inhibition ◽  
Alkaline Condition ◽  
Discovery Studio ◽  
Hela Cell Lines ◽  
Antiproliferative Activities

Background: Spirocyclic indoline compounds widely exist in numerous natural products with good biological activities and some drug molecules in many aspects. In recent years, it has attracted extensive attention as potent anti-tumor agents in the fields of pharmacology and chemistry. Objective: In this study, we focused on designing and synthesizing a set of novel 1'-H-spiro[indole-3,4'-piperidine] derivatives, which were evaluated by preliminary bioactivity experiment in vitro and molecular docking. Method: The key intermediate 1'-methylspiro[indoline-3,4'-piperidine] (B4) reacted with benzenesulfonyl chloride with different substituents under alkaline condition to obtain its sulfonyl derivatives (B5-B10). We evaluated their antiproliferative activities against A549, BEL-7402 and HeLa cells by MTT assay. We performed the CDOCKER module in Discovery Studio 2.5.5 software for molecular modeling of compound B5, and investigated the binding of compound B5 with the target proteins from PDB database. Results: The results indicated that compounds B4-B10 exhibited good antiproliferative activities against the above three types of cells, in which compound B5 with chloride atom as electron-withdrawing substituent on a phenyl ring showed the highest potency against BEL-7402 cells (IC50=30.03±0.43 μg/mL). By binging of the prominent bioactive compound B5 to CDK, c-Met, EGFR protein crystals, The binding energy of B5 with these three types receptors are -44.3583 kcal/mol, - 38.3292 kcal/mol, -33.3653 kcal/mol respectively. Conclusion: Six 1'-methylspiro[indoline-3,4'-piperidine] derivatives were synthesized and evaluated against BEL-7402, A- 549, HeLa cell lines. Compound B5 showed significant inhibition on BEL-7402 cell lines. Molecular docking revealed that B5 showed good affinity by the good fitting between B5 and these three targets with amino acid residues in active sites which encourage us to conduct further evaluation such as the kinase experiment.

Synthesis and Cytotoxicity of New Mannich Bases of 6-[3-(3,4,5-Trimetoxyphenyl)-2- propenoyl]-2(3H)-Benzoxazolone

2020 ◽  
Vol 17 (4) ◽  
pp. 512-517
Author(s):  
Ognyan Ivanov Petrov ◽  
Yordanka Borisova Ivanova ◽  
Mariana Stefanova Gerova ◽  
Georgi Tsvetanov Momekov
Keyword(s):  
Tumor Cell ◽  
Cell Lines ◽  
Biological Activities ◽  
Human Tumor ◽  
Mannich Bases ◽  
In Vitro Cytotoxicity ◽  
Tumor Cell Lines ◽  
Human Tumor Cell ◽  
Human Tumor Cell Lines

Background: Chemotherapy is one of the mainstays of cancer treatment, despite the serious side effects of the clinically available anticancer drugs. In recent years increasing attention has been directed towards novel agents with improved efficacy and selectivity. Compounds with chalcone backbone have been reported to possess various biological activities such as anticancer, antimicrobial, anti-inflammatory, analgesic, antioxidant, etc. It was reported that aminomethylation of hydroxy chalcones to the corresponding Mannich bases increased their cytotoxicity. In this context, our interest has been focused on the design and synthesis of the so-called multi-target molecules, containing two or more pharmacophore fragments. Methods: A series of Mannich bases were synthesized by the reaction between 6-[3-(3,4,5- trimethoxyphenyl)-2-propenoyl]-2(3Н)-benzoxazolone, formaldehyde, and a secondary amine. The structures of the compounds were confirmed by elemental analysis, IR and NMR spectra. The new Mannich bases were evaluated for their in vitro cytotoxicity against a panel of human tumor cell lines, including BV-173, SKW-3, K-562, HL-60, HD-MY-Z and MDA-MB-231. The effects of selected compounds on the cellular levels of glutathione (GSH) were determined. Results: The new compounds 4a-e exhibited concentration-dependent cytotoxic effects at micromolar concentrations in MTT-dye reduction assay against a panel of human tumor cell lines, similar to those of starting chalcone 3. The tested agents led to concentration - dependent depletion of cellular GSH levels, whereby the effects of the chalcone prototype 3 and its Mannich base-derivatives were comparable. Conclusion: The highest chemosensitivity to the tested compounds was observed in BV- 173followed by SKW-3 and HL-60 cell lines.

Influence of New Synthetic Xanthones on the Proliferation and Migration Potential of Cancer Cell Lines In Vitro

2020 ◽  
Vol 19 (16) ◽  
pp. 1949-1965 ◽  
Author(s):  
Natalia Szkaradek ◽  
Daniel Sypniewski ◽  
Dorota Żelaszczyk ◽  
Sabina Gałka ◽  
Paulina Borzdziłowska ◽  
...  
Keyword(s):  
Cancer Cells ◽  
Cell Lines ◽  
Cancer Cell ◽  
Higher Plants ◽  
Biological Activities ◽  
Human Tumor ◽  
Plant Metabolites ◽  
Xtt Assay ◽  
Treatment Protocols

Background: Natural plant metabolites and their semisynthetic derivatives have been used for years in cancer therapy. Xanthones are oxygenated heterocyclic compounds produced as secondary metabolites by higher plants, fungi or lichens. Xanthone core may serve as a template in the synthesis of many derivatives that have broad biological activities. Objective: This study synthesized a series of 17 new xanthones, and their anticancer potential was also evaluated. Methods: The anticancer potential was evaluated in vitro using a highly invasive T24 cancer cell line. Direct cytotoxic effects of the xanthones were established by IC50 estimation based on XTT assay. Results: 5 compounds of the total 17 showed significant cytotoxicity toward the studied cancer cultures and were submitted to further detailed analysis, including studies examining their influence on gelatinase A and B expression, as well as on the cancer cells migration and adhesion to an extracellular matrix. These analyses were carried out on five human tumor cell lines: A2780 (ovarian cancer), A549 (lung cancer), HeLa (cervical cancer), Hep G2 (liver cancer), and T24 (urinary bladder cancer). All the compounds, especially 4, showed promising anticancer activity: they exhibited significant cytotoxicity towards all the evaluated cell lines, including MCF-7 breast cancer, and hindered migration-motility activity of cancer cells demonstrating more potent activity than α-mangostin which served as a reference xanthone. Conclusion: These results suggest that our xanthone derivatives may be further analyzed in order to include them in cancer treatment protocols.

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