Benzoin Schiff Bases: Design, Synthesis, and Biological Evaluation as Potential Antitumor Agents

Sabbah, Dima A.; Al-Tarawneh, Fatima; Talib, Wamidh H.; Sweidan, Kamal; Bardaweel, Sanaa K.; Al‐Shalabi, Eveen; Zhong, Haizhen A.; Sheikha, Ghassan Abu; Khalaf, Reema Abu; Mubarak, Mohammad S.

doi:10.2174/1573406414666180412160142

Cited by 22 publications

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“…The difference in activity between 12 and 27 might be due to the H bond supplied by the O atom. It is worth noting that the series exhibited distinct antiproliferative activity in both cell lines, suggesting differences in the binding sites of WT PI3Kα and MUT (H1047R) PI3Kα, which accords with our previous data on PI3Kα [13,14,[16][17][18][19]23,24].…”

Section: Biological Evaluation Of the Synthesized Compoundssupporting

confidence: 91%

“…Lately, we released a series of N-substituted 4-hydroxy-2-quinolone-3-carboxamides that suppressed human colon carcinoma (HCT116) cell line proliferation and enhanced apoptosis through inducing caspase-3 activity and destructing cellular DNA illustrated by 3 [18]. Our ceaseless research has uncovered diverse scaffolds [19][20][21][22][23][24] targeting PI3Kα.…”

Section: Introductionmentioning

confidence: 99%

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Molecular Modeling, Synthesis and Biological Evaluation of N-Phenyl-4-Hydroxy-6-Methyl-2-Quinolone-3-CarboxAmides as Anticancer Agents

et al. 2020

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The emergence of phosphatidylinositol 3-kinase (PI3Kα) in cancer development has accentuated its significance as a potential target for anticancer drug design. Twenty one derivatives of N-phenyl-4-hydroxy-6-methyl-2-quinolone-3-carboxamide were synthesized and characterized using NMR (1H and 13C) and HRMS. The derivatives displayed inhibitory activity against human epithelial colorectal adenocarcinoma (Caco-2) and human colon cancer (HCT-116) cell lines: compounds 8 (IC50 Caco-2 = 98 µM, IC50 HCT-116 = 337 µM) and 16 (IC50 Caco-2 = 13 µM, IC50 HCT-116 = 240.2 µM). Results showed that compound 16 significantly affected the gene encoding AKT, BAD, and PI3K. The induced-fit docking (IFD) studies against PI3Kα demonstrated that the scaffold accommodates the kinase domains and forms H-bonds with significant binding residues.

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Section: Biological Evaluation Of the Synthesized Compoundssupporting

confidence: 91%

Section: Introductionmentioning

confidence: 99%

Molecular Modeling, Synthesis and Biological Evaluation of N-Phenyl-4-Hydroxy-6-Methyl-2-Quinolone-3-CarboxAmides as Anticancer Agents

et al. 2020

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“…After 24 h, the media in each well were removed and then the attached cells were treated in triplicate with H. orientalis L. different extracts (initially dissolved in 0.1% DMSO). Using serial dilution technique, the extract and fractions were added in concentrations between 50-0.78 mg/mL and re-incubated for 48 h. Cell viability was measured using MTT [3-(4,5-Dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide] assay kit (Sigma, USA) as previously described [40]. Briefly, after 48 h incubation with 100 µL of extracts and fractions, media was removed from each well and 10 µL MTT was added.…”

Section: Antiproliferative Assaymentioning

confidence: 99%

“…Foldincrease in caspase-3 activity was detected by comparing extracts results with the level of the negative control. Procedure of the assay was carried out as described previously [40].…”

Section: Apoptosis Detection In T47d Cellsmentioning

confidence: 99%

Immunomodulatory and Anticancer Activities of Hyacinthus orientalis L.: An In Vitro and In Vivo Study

Kury

Taha

Talib

2021

Plants

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Hyacinthus orientalis L. (family Hyacinthaceae) is traditionally used to treat different diseases including cancer. In this study, the anticancer and immunomodulatory effects of this plant were evaluated. Hydroalcoholic extract was prepared, and different solvent fractions were obtained using solvent–solvent extraction. In the anticancer part, MTT assay and caspase-3 ELISA kits were used to measure the antiproliferative and apoptosis induction ability for each extract, respectively. In the immunomodulatory part, lymphocyte proliferation assay and cytokines detection kit were used to measure the effect of extracts of acquired immunity. Phagocytosis and pinocytosis induction were used to evaluate the effect of extracts on the innate immunity. GC–MS, LC–MS, and Foline–Ciocalteu assays were used to identify the chemical composition of the plant. Balb/C mice were inoculated with breast cancer and treated with hydroalcoholic extract of H. orientalis L. Results showed that hydroalcoholic extract and n-hexane fraction were highly effective in apoptosis induction. Both extract and fraction were also effective in stimulating lymphocytes proliferation and phagocytosis. Significant reduction in tumor size was achieved after treating tumor-bearing mice with hydroalcoholic extract. Additionally, high cure percentages (50%) were obtained in treated mice. Results of this study showed that H. orientalis L. has promising anticancer and immunomodulatory activities. However, further studies are needed to explore more details of apoptosis induction ability and other mechanisms of action and to measure different signaling pathways responsible for the anticancer and immunomodulatory response.

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“…After 24 h, the media in each well were completely removed and the attached cells were treated in triplicates with decreasing concentrations of different extracts (initially dissolved in DMSO) of T. boudieri (25-0.78 mg/ml. Plates were incubated for 48 h, and then cell viability was measured by using MTT [3-(4,5-Dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide] assay kit (Sigma, USA) assay as previously described (20). Percentage survival was calculated by comparing the absorbance of treated cells to that of untreated cells (tissue culture media + 0.1% DMSO).…”

Section: Antiproliferative Assaymentioning

confidence: 99%

Terfezia boudieri: A Desert Truffle With Anticancer and Immunomodulatory Activities

Obaydi

Hamed²,

Kury

et al. 2020

Front. Nutr.

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Desert truffles have high nutritional value and grow wild in the Mediterranean basin and Western Asia. Although, many studies were performed to evaluate truffles nutritious values and phytochemical composition, studies are limited to evaluate their anticancer and/ or immunomodulatory effects. Our study was conducted to evaluate the anticancer and immunomodulatory effects of Terfezia boudieri (desert truffle). Different solvent extracts were prepared from the truffle and MTT assay was used to measure their anticancer activity against cancer cell lines (T47D, MCF-7, MDA-MB231, HCT-116, and Hela). Total phenolic content in each extract was determined by using Folin-Ciocalteu reagent and qualitative phytochemical screening was performed using standard methods. The degree of apoptosis induction (using caspase 3 assay) and vascular endothelial growth factor expression were detected using standard kits. Also, ELISA was used to measure levels of IFN-γ, IL-2, IL-4, and IL-10 secreted by splenocytes after treatment with the extracts. The effect of the extracts on splenocytes proliferation was measured using MTT assay. Macrophage function was evaluated using nitro blue tetrazolium assay and pinocytosis function was evaluated using neutral red method. Terpenoids, phytosterols, and carbohydrates were present in all the solvent extracts, while tannins, alkaloids and flavonoids were detected only in aqueous/methanol and aqueous extracts. The highest total phenolic content was observed in aqueous and aqueous methanol extracts. The growth of cancer cell lines was inhibited by T. boudieri extracts in a dose dependent manner. N-hexane extract was the most potent against most cell lines. Aqueous/methanol extract showed high apoptosis induction and angiogenesis suppression effects. An increase in TH1 cytokines (IFN-γ, IL-2) level and a decrease in TH2 cytokine (IL-4) level were evident after lymphocytes stimulation by aqueous/methanol, n-hexane and ethyl acetate extracts of T. boudieri. Ethyl acetate extract of T. boudieri were the most potent extracts to stimulate lymphocytes proliferation while all other extracts showed moderate stimulation. Aqueous/methanol extract was the most active extract to stimulate phagocytosis. Ethyl acetate extract was the most active extract to stimulate pinocytosis. The use of T. boudieri provides variable health benefits. N-hexane, ethyl acetate, and aqueous/methanol extracts exhibited anticancer activities and are potent stimulators of innate and acquired immunity. Further testing is needed to identify the biologically active compounds and detect them quantitatively using GC-MS analysis.

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Benzoin Schiff Bases: Design, Synthesis, and Biological Evaluation as Potential Antitumor Agents

Abstract: The series exerted a potential PI3Kα inhibitory activity in human carcinoma cell lines expressing PI3Kα.

Cited by 22 publications

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Molecular Modeling, Synthesis and Biological Evaluation of N-Phenyl-4-Hydroxy-6-Methyl-2-Quinolone-3-CarboxAmides as Anticancer Agents

Molecular Modeling, Synthesis and Biological Evaluation of N-Phenyl-4-Hydroxy-6-Methyl-2-Quinolone-3-CarboxAmides as Anticancer Agents

Immunomodulatory and Anticancer Activities of Hyacinthus orientalis L.: An In Vitro and In Vivo Study

Terfezia boudieri: A Desert Truffle With Anticancer and Immunomodulatory Activities

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