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  1. Article ; Online: Synthesis and molecular docking of some new thiazolidinone and thiadiazole derivatives as anticancer agents.

    Saeed, Ali / Soliman, Ahbarah M / Abdullah, Mahmood M S / Abdel-Latif, Ehab / El-Demerdash, Amr

    Chemistry & biodiversity

    2024  , Page(s) e202301870

    Abstract: New sets of functionalized thiazolidinone and thiadiazole derivatives were synthesized, and their cytotoxicity was evaluated on HepG2, MCF-7, HTC-116, and WI38 cells. The synthetic approach is based on the preparation of 4-(4-acetamidophenyl) ... ...

    Abstract New sets of functionalized thiazolidinone and thiadiazole derivatives were synthesized, and their cytotoxicity was evaluated on HepG2, MCF-7, HTC-116, and WI38 cells. The synthetic approach is based on the preparation of 4-(4-acetamidophenyl)thiosemicarbazide (4) and their thiosemicarbazones 5a-e, which are converted to the corresponding thiazoldin-4-one compounds 6a-e upon cyclization with ethyl bromoacetate. The thiadiazole compounds 9 and 12 were obtained by reacting 4-(4-acetamidophenyl)thiosemicarbazide with isothiocyanates and/or ethyl 2-cyano-3,3-bis(methylthio)acrylate, respectively. The thiazolidinone compounds 6c and 6e exhibited strong cytotoxicity against breast cancer cells, with an IC50 (6.70±0.5 µM) and IC50 (7.51±0.8 µM), respectively, very close to that of doxorubicin (IC50: 4.17±0.2 µM). In addition, the anti-cancer properties of the tested thiazolidinone and thiadiazole scaffolds were further explored by the molecular docking program (MOE)-(PDB Code-1DLS). Compounds 5d, 5e, 6d, 6e, and 7 have the best binding affinity, ranging from -8.5386 kcal.mol-1 to -8.2830 kcal.mol-1.
    Language English
    Publishing date 2024-03-27
    Publishing country Switzerland
    Document type Journal Article
    ZDB-ID 2139001-0
    ISSN 1612-1880 ; 1612-1872
    ISSN (online) 1612-1880
    ISSN 1612-1872
    DOI 10.1002/cbdv.202301870
    Database MEDical Literature Analysis and Retrieval System OnLINE

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  2. Article ; Online: Chemical Diversity and Biological Activities of

    El-Demerdash, Amr

    Journal of fungi (Basel, Switzerland)

    2018  Volume 4, Issue 4

    Abstract: Microbial natural products (MNPs) have been identified as important hotspots and effective sources for drug lead discovery. The ... ...

    Abstract Microbial natural products (MNPs) have been identified as important hotspots and effective sources for drug lead discovery. The genus
    Language English
    Publishing date 2018-12-05
    Publishing country Switzerland
    Document type Journal Article ; Review
    ZDB-ID 2784229-0
    ISSN 2309-608X ; 2309-608X
    ISSN (online) 2309-608X
    ISSN 2309-608X
    DOI 10.3390/jof4040130
    Database MEDical Literature Analysis and Retrieval System OnLINE

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  3. Article ; Online: Recent advances in the discovery, biosynthesis, and therapeutic potential of isocoumarins derived from fungi: a comprehensive update.

    Tammam, Mohamed A / Gamal El-Din, Mariam I / Abood, Amira / El-Demerdash, Amr

    RSC advances

    2023  Volume 13, Issue 12, Page(s) 8049–8089

    Abstract: Microorganisms still remain the main hotspots in the global drug discovery avenue. In particular, fungi are highly prolific producers of vast structurally diverse specialized secondary metabolites, which have displayed a myriad of biomedical potentials. ... ...

    Abstract Microorganisms still remain the main hotspots in the global drug discovery avenue. In particular, fungi are highly prolific producers of vast structurally diverse specialized secondary metabolites, which have displayed a myriad of biomedical potentials. Intriguingly, isocoumarins is one distinctive class of fungal natural products polyketides, which demonstrated numerous remarkable biological and pharmacological activities. This review article provides a comprehensive state-of-the-art over the period 2000-2022 about the discovery, isolation, classifications, and therapeutic potentials of isocoumarins exclusively reported from fungi. Indeed, a comprehensive list of 351 structurally diverse isocoumarins were documented and classified according to their fungal sources [16 order/28 family/55 genera] where they have been originally discovered along with their reported pharmacological activities wherever applicable. Also, recent insights around their proposed and experimentally proven biosynthetic pathways are also briefly discussed.
    Language English
    Publishing date 2023-03-10
    Publishing country England
    Document type Journal Article ; Review
    ISSN 2046-2069
    ISSN (online) 2046-2069
    DOI 10.1039/d2ra08245d
    Database MEDical Literature Analysis and Retrieval System OnLINE

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  4. Article ; Online: Investigating the antiviral therapeutic potentialities of marine polycyclic lamellarin pyrrole alkaloids as promising inhibitors for SARS-CoV-2 and Zika main proteases (Mpro).

    Pereira, Florbela / Bedda, Loay / Tammam, Mohamed A / Alabdullah, Abdul Kader / Arafa, Reem / El-Demerdash, Amr

    Journal of biomolecular structure & dynamics

    2023  Volume 42, Issue 8, Page(s) 3983–4001

    Abstract: The new coronavirus variant (SARS-CoV-2) and Zika virus are two world-wide health pandemics. Along history, natural products-based drugs have always crucially recognized as a main source of valuable medications. Considering the SARS-CoV-2 and Zika main ... ...

    Abstract The new coronavirus variant (SARS-CoV-2) and Zika virus are two world-wide health pandemics. Along history, natural products-based drugs have always crucially recognized as a main source of valuable medications. Considering the SARS-CoV-2 and Zika main proteases (
    MeSH term(s) Molecular Docking Simulation ; SARS-CoV-2/drug effects ; SARS-CoV-2/enzymology ; Alkaloids/chemistry ; Alkaloids/pharmacology ; Zika Virus/enzymology ; Zika Virus/drug effects ; Antiviral Agents/pharmacology ; Antiviral Agents/chemistry ; Molecular Dynamics Simulation ; Humans ; Structure-Activity Relationship ; COVID-19/virology ; Pyrroles/chemistry ; Pyrroles/pharmacology ; Protease Inhibitors/chemistry ; Protease Inhibitors/pharmacology ; Protein Binding ; Betacoronavirus/drug effects ; Betacoronavirus/enzymology ; Aquatic Organisms ; Pandemics ; Binding Sites
    Chemical Substances Alkaloids ; Antiviral Agents ; Pyrroles ; Protease Inhibitors
    Language English
    Publishing date 2023-05-26
    Publishing country England
    Document type Journal Article
    ZDB-ID 49157-3
    ISSN 1538-0254 ; 0739-1102
    ISSN (online) 1538-0254
    ISSN 0739-1102
    DOI 10.1080/07391102.2023.2217513
    Database MEDical Literature Analysis and Retrieval System OnLINE

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  5. Article ; Online: Chemical Diversity and Biological Activities of Phaeosphaeria Fungi Genus

    Amr El-Demerdash

    Journal of Fungi, Vol 4, Iss 4, p

    A Systematic Review

    2018  Volume 130

    Abstract: Microbial natural products (MNPs) have been identified as important hotspots and effective sources for drug lead discovery. The genus Phaeosphaeria (family: Phaeosphaeriaceae, order: Pleosporales), in particular, has produced divergent chemical ... ...

    Abstract Microbial natural products (MNPs) have been identified as important hotspots and effective sources for drug lead discovery. The genus Phaeosphaeria (family: Phaeosphaeriaceae, order: Pleosporales), in particular, has produced divergent chemical structures, including pyrazine alkaloids, isocoumarins, perylenequinones, anthraquinones, diterpenes, and cyclic peptides, which display a wide scope of biological potentialities. This contribution comprehensively highlights, over the period 1974⁻2018, the chemistry and biology of the isolated natural products from the micro-filamentous Phaeosphaeria fungi genus. A list of 71 compounds, with structural and biological diversities, were gathered into 5 main groups.
    Keywords Phaeosphaeria ; pyrazine alkaloids ; polyketides ; isocoumarins ; perylenequinones ; anthraquinones ; cyclic peptides ; bioactivities ; Biology (General) ; QH301-705.5
    Language English
    Publishing date 2018-12-01T00:00:00Z
    Publisher MDPI AG
    Document type Article ; Online
    Database BASE - Bielefeld Academic Search Engine (life sciences selection)

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  6. Article ; Online: Investigating the hepatoprotective potentiality of marine-derived steroids as promising inhibitors of liver fibrosis.

    Tammam, Mohamed A / Pereira, Florbela / Aly, Omnia / Sebak, Mohamed / Diab, Yasser M / Mahdy, Aldoushy / El-Demerdash, Amr

    RSC advances

    2023  Volume 13, Issue 39, Page(s) 27477–27490

    Abstract: It has been reported that organic extracts derived from soft corals belonging to the ... ...

    Abstract It has been reported that organic extracts derived from soft corals belonging to the genus
    Language English
    Publishing date 2023-09-13
    Publishing country England
    Document type Journal Article
    ISSN 2046-2069
    ISSN (online) 2046-2069
    DOI 10.1039/d3ra04843h
    Database MEDical Literature Analysis and Retrieval System OnLINE

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  7. Article: Cytotoxic constituents from the wheat plant pathogen Parastagonospora nodorum SN15

    El-Demerdash, Amr / Borde, Chloé / Genta-Jouve, Gregory / Escargueil, Alexandre / Prado, Soizic

    Natural product research. 2022 Mar. 4, v. 36, no. 5

    2022  

    Abstract: Microbial natural products are continuing to be a promising platform for future drug lead discover. As a part of our ongoing research program on fungal natural product, herein we report metabolites isolated from the fungus Parastagonospora nodorum SN15 a ...

    Abstract Microbial natural products are continuing to be a promising platform for future drug lead discover. As a part of our ongoing research program on fungal natural product, herein we report metabolites isolated from the fungus Parastagonospora nodorum SN15 a pathogen of wheat and related cereals. Its chemical investigation led to the purification of new isoleucinic acid derivatives (1–2) along with the cis procuramine (4). Their structures were determined based on extensive NMR and the relative configuration by comparison of experimental and predicted NMR chemical shifts. All compounds were evaluated for their cytotoxic activity against a panel of human cell lines and some displayed specific feature towards cancer cells compared to normal immortalised fibroblasts.
    Keywords Parastagonospora nodorum ; cytotoxicity ; fibroblasts ; fungi ; humans ; metabolites ; plant pathogens ; research programs ; wheat
    Language English
    Dates of publication 2022-0304
    Size p. 1273-1281.
    Publishing place Taylor & Francis
    Document type Article
    ZDB-ID 2185747-7
    ISSN 1478-6427 ; 1478-6419
    ISSN (online) 1478-6427
    ISSN 1478-6419
    DOI 10.1080/14786419.2021.1877702
    Database NAL-Catalogue (AGRICOLA)

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  8. Article ; Online: Chemical Diversity and Biological Activities of Meroterpenoids from Marine Derived-Fungi: A Comprehensive Update.

    El-Demerdash, Amr / Kumla, Decha / Kijjoa, Anake

    Marine drugs

    2020  Volume 18, Issue 6

    Abstract: Meroterpenoids are a class of hybrid natural products, partially derived from a mixed terpenoid pathway. They possess remarkable structural features and relevant biological and pharmacological activities. Marine-derived fungi are a rich source of ... ...

    Abstract Meroterpenoids are a class of hybrid natural products, partially derived from a mixed terpenoid pathway. They possess remarkable structural features and relevant biological and pharmacological activities. Marine-derived fungi are a rich source of meroterpenoids featuring structural diversity varying from simple to complex molecular architectures. A combination of a structural variability and their myriad of bioactivities makes meroterpenoids an interesting class of naturally occurring compounds for chemical and pharmacological investigation. In this review, a comprehensive literature survey covering the period of 2009-2019, with 86 references, is presented focusing on chemistry and biological activities of various classes of meroterpenoids isolated from fungi obtained from different marine hosts and environments.
    MeSH term(s) Aquatic Organisms/chemistry ; Biological Products/chemistry ; Biological Products/isolation & purification ; Biological Products/pharmacology ; Fungi/chemistry ; Molecular Structure ; Terpenes/chemistry ; Terpenes/isolation & purification ; Terpenes/pharmacology
    Chemical Substances Biological Products ; Terpenes
    Language English
    Publishing date 2020-06-15
    Publishing country Switzerland
    Document type Journal Article ; Review
    ZDB-ID 2175190-0
    ISSN 1660-3397 ; 1660-3397
    ISSN (online) 1660-3397
    ISSN 1660-3397
    DOI 10.3390/md18060317
    Database MEDical Literature Analysis and Retrieval System OnLINE

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  9. Article ; Online: Chemical diversity, medicinal potentialities, biosynthesis, and pharmacokinetics of anthraquinones and their congeners derived from marine fungi: a comprehensive update.

    Sebak, Mohamed / Molham, Fatma / Greco, Claudio / Tammam, Mohamed A / Sobeh, Mansour / El-Demerdash, Amr

    RSC advances

    2022  Volume 12, Issue 38, Page(s) 24887–24921

    Abstract: Marine fungi receive excessive attention as prolific producers of structurally unique secondary metabolites, offering promising potential as substitutes or conjugates for current therapeutics, whereas existing research has only scratched the surface in ... ...

    Abstract Marine fungi receive excessive attention as prolific producers of structurally unique secondary metabolites, offering promising potential as substitutes or conjugates for current therapeutics, whereas existing research has only scratched the surface in terms of secondary metabolite diversity and potential industrial applications as only a small share of bioactive natural products have been identified from marine-derived fungi thus far. Anthraquinones derived from filamentous fungi are a distinct large group of polyketides containing compounds which feature a common 9,10-dioxoanthracene core, while their derivatives are generated through enzymatic reactions such as methylation, oxidation, or dimerization to produce a large variety of anthraquinone derivatives. A considerable number of reported anthraquinones and their derivatives have shown significant biological activities as well as highly economical, commercial, and biomedical potentialities such as anticancer, antimicrobial, antioxidant, and anti-inflammatory activities. Accordingly, and in this context, this review comprehensively covers the state-of-art over 20 years of about 208 structurally diverse anthraquinones and their derivatives isolated from different species of marine-derived fungal genera along with their reported bioactivity wherever applicable. Also, in this manuscript, we will present in brief recent insights centred on their experimentally proved biosynthetic routes. Moreover, all reported compounds were extensively investigated for their
    Language English
    Publishing date 2022-09-01
    Publishing country England
    Document type Journal Article ; Review
    ISSN 2046-2069
    ISSN (online) 2046-2069
    DOI 10.1039/d2ra03610j
    Database MEDical Literature Analysis and Retrieval System OnLINE

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  10. Article ; Online: SYNTHESIS OF SOME NOVEL THIOPHENE ANALOGUES AS POTENTIAL ANTICANCER AGENTS.

    Almatari, Altaf S / Saeed, Ali / Abdel-Ghani, Ghada E / Abdullah, Mahmood M S / Al-Lohedan, Hamad A / Abdel-Latif, Ehab / El-Demerdash, Amr

    Chemistry & biodiversity

    2024  , Page(s) e202400313

    Abstract: The aim of this study involves the synthesis novel thiophene analogues that can be used as anticancer medications through a strategic multicomponent reaction connecting ethyl 4-chloroacetoacetate (1), phenyl isothiocyanate, and a series of active ... ...

    Abstract The aim of this study involves the synthesis novel thiophene analogues that can be used as anticancer medications through a strategic multicomponent reaction connecting ethyl 4-chloroacetoacetate (1), phenyl isothiocyanate, and a series of active methylene reagents, including ethyl acetoacetate (2), malononitrile, ethyl cyanoacetate, cyanoacetamide 6a-c, N-phenyl cyanoacetamide derivatives 13a-c, and acetoacetanilide derivatives 18. This reaction was facilitated by dry dimethylformamide with a catalytic quantity of K2CO3. The resultant thiophene derivatives were identified as 4, 8a-b, 9, 12a-d, 15a-c, and 20a-b. Further reaction of compound 4 with hydrazine hydrate yielded derivative 5, respectively. When compound 1 was refluxed with ethyl 3-mercapto-3-(phenylamino)-2-(p-substituted phenyldiazenyl)acrylate 10a-e in the presence of sodium ethoxide, it produced thiophene derivatives 12a-d. Comprehensive structural elucidation of these newly synthesized thiophene-analogues was accomplished via elemental and spectral analysis data. Furthermore, the study delves into the cytotoxicity of the newly synthesized thiophenes was evaluated using the HepG2, A2780, and A2780CP cell lines. The amino-thiophene derivative 15b exhibited an increased growth inhibition of A2780, and A2780CP with IC50 values 12±0.17, and 10±0.15 µM, respectively compared to Sorafenib with IC50 values 7.5±0.54 and 9.4±0.14. This research opens new avenues for developing thiophene-based anticancer agents.
    Language English
    Publishing date 2024-03-11
    Publishing country Switzerland
    Document type Journal Article
    ZDB-ID 2139001-0
    ISSN 1612-1880 ; 1612-1872
    ISSN (online) 1612-1880
    ISSN 1612-1872
    DOI 10.1002/cbdv.202400313
    Database MEDical Literature Analysis and Retrieval System OnLINE

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