Synthesis and Antitumor Evaluation of New Heterocycles Derived from 3-Methyl-2-benzothiazolinone Hydrazone

Ibrahim, Nabila M.; Yosef, Hisham Abdallah A.; Ewies, Ewies F.; Mahran, M. R.; Ali, Mamdouh M.; Mahmoud, Abeer E.

doi:10.5935/0103-5053.20150071

Cited by 4 publications

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“…The anticancer activity of UFOP and FOP methanolic extracts (which had maximum total phenolic recovery and the highest antioxidant activity among other solvents used in the study) was measured as described by Skehan et al, (1990) and Ibrahim et al, (2015) using the Sulfo-Rhodamine-B stain assay. Cells were incubated with serial dilutions of UFOP and FOP extracts or the reference drug doxorubicin for 48 h. Then the cells were stained with 0.4% acetic acid SRB solution.…”

Section: In Vitro Anticancer Activity Assay Of Ufop and Fop Methanolimentioning

confidence: 99%

Antioxidant and anticancer efficacy of therapeutic bioactive compounds from fermented olive waste

et al. 2018

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Olive pomace, which is considered as one of the worst agro-industrial wastes in Mediterranean countries was tested for bioactive compounds production through the solid state fermentation of Kluyveromyces marxianus. Because they present potent biological activities, phenolic compounds from both unfermented and fermented pomace were extracted with simultaneous evaluation of their antioxidant and anticancer activities. Conditions for optimum total phenolic recovery with maximum antioxidant activity were optimized using methanol as the extracting solvent with a sample to solvent ratio of 1:10 at 50 °C for 2 hours. The in-vitro anticancer activity of both extracts was assessed against different human cancer cell lines. The results revealed that both extracts exerted anticancer effects close to the value of doxorubicin drug against liver HepG2 and breast MCF-7 cell lines, and moderate activity against prostate PC3 and colon HCT116 cell lines. Nevertheless, the fermented extract was more potent than the unfermented one. No effect against lung A549, cervix Hela cancer cell lines or normal HFB4 cells was observed for both extracts. A GC/MS analysis was carried out to determine the compounds responsible for antioxidant and anticancer activities. The results showed the presence of methyl palmitate, methyl oleate, and ethyl oleate in the methanolic extract of unfermented olive pomace, while that of the fermented one showed the production of carvacrol, thymol, eugenol, caryophyllene oxide and methyl isopalmitate.

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Section: In Vitro Anticancer Activity Assay Of Ufop and Fop Methanolimentioning

confidence: 99%

Antioxidant and anticancer efficacy of therapeutic bioactive compounds from fermented olive waste

et al. 2018

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“…Some metal complexes have been reported to be more effective than their parent ligand, such as bleomycin (Li-June, 2003). Many biologically active compounds used as drugs possess enhanced modified pharmacological and toxicological potentials when administered in the form of metal-based compounds (Ibrahim et al, 2015;Babamale et al, 2016). More research has been carried out on the application of antimalaria drug metal complexes which has which are more recognized as a leading candidate for the treatment of different infectious diseases (Padman et al, 2016).…”

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Synthesis, Characterization, Antimalarial and Antimicrobial activities of Mixed Ibuprofen-Pyrimethamine M(II) Complexes [M = Cd, Co, Zn, Mn]

Bamigboye

Ejidike²

2019

Natural and Applied Sciences Journal

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Mixed complexes of Ibuprofen-Pyrimethamine were synthesized using Cd(II) Co(II), Zn(II), and Mn(II). The mixed complexes were characterized based on some physicochemical and spectroscopic techniques such as infrared, elemental analysis, conductivity measurements, and magnetic moment. Based on the results obtained, the complexes were formulated as [M(L1)(L2)]Cl2, where M = metal ion, L1 = Pyrimethamine, L2 = Ibuprofen). The complexes were found to be non-electrolytes. The ligands act as bidentate towards the central metal ions with deprotonation occurring at the carboxylic group. The complexes were also analyzed by conductometric titration. Antimicrobial screening against the selected organisms: Escherichia coli, Pseudomonas aeruginosa, Staphylococcus aureus, Bacillus substilis, Bacillus megaterium and Serratia marcescens for the complexes alongside the free ligands were investigated. The antimalarial study was investigated for the compounds against Plasmodium berghei (NK 65 strain). It was observed that the complexes showed significant potentials against the studied organisms.

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“…Accordingly, and in continuation of our ongoing research (Boulos et al, 2013a;El-Sayed et al, 2016;Ewies et al, 2014;Ewies et al, 2015;Ewies et al, 2016a;Ewies et al, 2016b;Ewies et al, 2019;Ibrahim et al, 2015, El-Husseiny et al, 2020El-Sayed et al, 2020) toward obtaining new compounds as promising biological activities and based on F I G U R E 2 Design of target compounds 5a-j, 6a,b, 7a-e, and 8a-f the previously reported findings regarding the biological activity of benzofuran and indole nucleus, we focused our attention on exploring the possibility of replacement of the 3,4,5-trimethoxybenzoyl moiety at position 2 of compound IV with a fluoro or trifluoromethyl substituted phenyl diazinyl moiety as in compounds 5a-j, 6a,b, and 8a-f. Both fluorine substituent or trifluoromethyl group are known to induce high effect on the binding affinity and increase stability of cell membrane as well as its permeability against metabolic oxidation (Usachev et al, 2008;Usachev et al, 2012).…”

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confidence: 61%

Design, synthesis, biological evaluation, and molecular docking of new benzofuran and indole derivatives as tubulin polymerization inhibitors

El‐Sayed

El‐Hussieny

Ewies

et al. 2021

Drug Development Research

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Microtubules and the mitotic spindle have become an important target for cancer treatment due to their critical role in cell division. In this work, a novel series of benzofuran and indole derivatives were designed and synthesized, to be evaluated as tubulin polymerization inhibitors. 2‐Acetylbenzofuran derivatives 1a,b and 3‐acetylindole 1c were condensed with Wittig reagents 2a–d and Wittig‐Horner reagents 3a–e to afford the respective 2‐ethylidene derivatives 5a–j and 7a–e. Also, iminomethylene triphenylphosphine (2e) reacted with 1a,b to afford benzofuran‐2‐ylethylidene aniline derivatives 6a,b. In addition, compounds 1a,b reacted with trialkylphosphites 4a–c to give 1:1 adduct for which the Oxaphospholo[4,3‐b]benzofuran‐7‐yl)diazene derivatives 8a–f, were assigned. The possible reactions mechanisms were discussed and structural reasoning for the new compounds were based upon spectroscopic data. Their antiproliferative activities against two cell lines namely, HepG2 and MCF7 cells were then evaluated. It was found that the benzofuran compounds 5b, 6a, and 8c exhibited the strongest antiproliferative activities against both cell lines compared to doxorubicin. By studying the mechanism of action, compound 6a showed good inhibition of tubulin polymerization which leads to mitotic spindle formation disruption, cell cycle arrest in the G2/M phase, and apoptosis of HepG2 cells. A conducted docking study confirmed the in vitro results indicating that compound 6a fitted properly at the colchicine binding site of tubulin. Based on these findings, compound 6a can be considered as a promising anticancer candidate that can be subjected for further development as a tubulin polymerization inhibitor for treating liver and breast cell carcinoma.

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Synthesis and Antitumor Evaluation of New Heterocycles Derived from 3-Methyl-2-benzothiazolinone Hydrazone

Cited by 4 publications

References 0 publications

Antioxidant and anticancer efficacy of therapeutic bioactive compounds from fermented olive waste

Antioxidant and anticancer efficacy of therapeutic bioactive compounds from fermented olive waste

Synthesis, Characterization, Antimalarial and Antimicrobial activities of Mixed Ibuprofen-Pyrimethamine M(II) Complexes [M = Cd, Co, Zn, Mn]

Design, synthesis, biological evaluation, and molecular docking of new benzofuran and indole derivatives as tubulin polymerization inhibitors

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