First Example of Cationic Cyclopentadienyliron Based Chromene Complexes and Polymers: Synthesis, Characterization, and Biological Applications

Abd‐El‐Aziz, Alaa S.; El-Ghezlani, Ebtehal G.; Elaasser, Mahmoud M.; Afifi, Tarek H.; Okasha, Rawda M.

doi:10.1007/s10904-019-01295-w

Cited by 14 publications

(8 citation statements)

References 51 publications

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“…As a result, compounds 56 and 57 (IC 50 15.6 and 29.3 μM) showed the remarkable cytotoxicity in the MCF-7 cell line. Also, SAR studies in this series might be helpful to identify the lead molecule from this series as an anticancer (Abd-El-Aziz et al, 2020 ).…”

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

confidence: 99%

“…The synthesized cationic organoiron complexes incorporated with chromenes were tested for their antimicrobial activities (methicillin-resistant S. aureus , vancomycin-resistant Enterococcus faecium and S. warnerii ). As a result, compounds 76 (IC 50 2.40 and 2.04 μM) exhibited considerable inhibition against S. aureus and S. warnerii , while compound 57 (IC 50 2.12 μM) showed the remarkable inhibition against E. faecium (Abd-El-Aziz et al, 2020 ).…”

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

confidence: 99%

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

confidence: 99%

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

confidence: 99%

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

2020

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“…Mccarroll and co-workers also reported that tephrosin, a viable anti-lung carcinoma drug, as well as Acronycine, a drug targeting colon, lung, and ovary tumors, obstruct the cell proliferation through their binding to the β-tubulin specific site, which subsequently induces apoptosis through microtubule polymerization [ 11 ]. Furthermore, chromene molecules are deemed ‘privileged medicinal scaffolds’ due to their unique pharmacological and biological activities [ 5 , 11 , 12 , 13 , 14 , 15 , 16 , 17 , 18 , 19 , 20 , 21 , 22 , 23 , 24 , 25 , 26 ].…”

Section: Introductionmentioning

confidence: 99%

A New Family of Benzo[h]Chromene Based Azo Dye: Synthesis, In-Silico and DFT Studies with In Vitro Antimicrobial and Antiproliferative Assessment

Abd‐El‐Aziz

Alsaggaf

Assirey

et al. 2021

IJMS

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The high biological activity of the chromene compounds coupled with the intriguing optical features of azo chromophores prompted our desire to construct novel derivatives of chromene incorporating azo moieties 4a-l, which have been prepared via a three-component reaction of 1-naphthalenol-4-[(4-ethoxyphenyl) azo], 1, with the benzaldehyde derivatives and malononitrile. The structural identities of the azo-chromene 4a-l were confirmed on the basis of their spectral data and elemental analysis, and a UV–visible study was performed in a Dimethylformamide (DMF) solution for these molecules. Additionally, the antimicrobial activity was investigated against four human pathogens (Gram-positive and Gram-negative bacteria) and four fungi, employing an agar well diffusion method, with their minimum inhibitory concentrations being reported. Molecules 4a, 4g, and 4h were discovered to be more efficacious against Syncephalastrum racemosum (RCMB 05922) in comparison to the reference drugs, while compounds 4b and 4h demonstrated the highest inhibitory activity against Escherichia coli (E. coli) in evaluation against the reference drugs. Moreover, their cytotoxicity was assessed against three different human cell lines, including human colon carcinoma (HCT-116), human hepatocellular carcinoma (HepG-2), and human breast adenocarcinoma (MCF-7) with a selection of molecules illustrating potency against the HCT-116 and MCF-7 cell lines. Furthermore, the molecular modeling results depicted the binding interactions of the synthesized compounds 3b and 3h in the active site of the E. coli DNA gyrase B enzyme with a clear SAR (structure–activity relationship) analysis. Lastly, the density functional theory’s (DFTs) theoretical calculations were performed to quantify the energy levels of the Frontier Molecular Orbitals (FMOs) and their energy gaps, dipole moments, and molecular electrostatic potentials. These data were utilized in the chemical descriptor estimations to confirm the biological activity.

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“…As a continuation of our preceding work in the area of the synthesis and biological screening of the bioactive molecules [19][20][21][22] based on extensive molecular modeling and in-silico studies, we carried out the synthesis of a novel series of chromene-incorporating flavanones, endeavoring to find new and alternative drug candidates to replace those in peril of facing resistance from microorganisms.…”

Section: Introductionmentioning

confidence: 99%

Synthesis, Biological Assessment, and Structure Activity Relationship Studies of New Flavanones Embodying Chromene Moieties

et al. 2020

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Novel flavanones that incorporate chromene motifs are synthesized via a one-step multicomponent reaction. The structures of the new chromenes are elucidated by using IR, 1H-NMR, 13C-NMR, 1H-1H COSY, HSQC, HMBC, and elemental analysis. The new compounds are screened for their in vitro antimicrobial and cytotoxic activities. The antimicrobial properties are investigated and established against seven human pathogens, employing the agar well diffusion method and the minimum inhibitory concentrations. A majority of the assessed derivatives are found to exhibit significant antimicrobial activities against most bacterial strains, in comparison to standard reference drugs. Moreover, their cytotoxicity is appraised against four different human carcinoma cell lines: human colon carcinoma (HCT-116), human hepatocellular carcinoma (HepG-2), human breast adenocarcinoma (MCF-7), and adenocarcinoma human alveolar basal epithelial cell (A-549). All the desired compounds are subjected to in-silico studies, forecasting their drug likeness, bioactivity, and the absorption, distribution, metabolism, and excretion (ADME) properties prior to their synthetic assembly. The in-silico molecular docking evaluation of all the targeted derivatives is undertaken on gyrase B and the cyclin-dependent kinase. The in-silico predicted outcomes were endorsed by the in vitro studies.

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First Example of Cationic Cyclopentadienyliron Based Chromene Complexes and Polymers: Synthesis, Characterization, and Biological Applications

Cited by 14 publications

References 51 publications

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

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

A New Family of Benzo[h]Chromene Based Azo Dye: Synthesis, In-Silico and DFT Studies with In Vitro Antimicrobial and Antiproliferative Assessment

Synthesis, Biological Assessment, and Structure Activity Relationship Studies of New Flavanones Embodying Chromene Moieties

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