Fusarithioamide B, a new benzamide derivative from the endophytic fungus Fusarium chlamydosporium with potent cytotoxic and antimicrobial activities

Ibrahim, Sabrin R. M.; Mohamed, Gamal A.; Haidari, Rwaida A. Al; Zayed, Mohamed F.; El-Kholy, Amal A.; Elkhayat, Ehab S.; Ross, Samir A.

doi:10.1016/j.bmc.2017.12.049

Cited by 58 publications

(38 citation statements)

References 22 publications

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“…The 2,3-disubstituted-6-fluoro-3 H -quinazolin-4-ones ( 6 – 8 ) and ( 10a – g ) were subjected to cytotoxic screening using two types of breast cancer cell lines (MCF-7) and (MDA-MBA-231) using MTT assay [ 17 , 18 , 19 ]. The IC 50 values of screening are listed in Table 1 .…”

Section: Resultsmentioning

confidence: 99%

“…20 µL of MTT was added to each well and incubated for 2 h before 200 µL DMSO was added. The absorbance was measured on an ELISA reader (Multiskan EX, Lab systems, Waltham, MA, USA) at wavelength of 570 nm [ 17 , 18 ].…”

Section: Methodsmentioning

confidence: 99%

“…Other quinazolines yield their anticancer activity by inhibition of DNA repairing system or tubulin polymerization. There are many other derivatives have dual EGFR/tubulin polymerization inhibitors, like amide derivatives and quinoxalines [ 16 , 17 , 18 , 19 ]. Many efforts have been aimed at finding safe and potent molecules with the present chemotherapeutic agents [ 10 , 11 , 12 , 13 , 14 , 15 ].…”

Section: Introductionmentioning

confidence: 99%

“…Moreover, Fluorine substitution could improve the overall pharmacokinetics and pharmacodynamics of the molecule by improving solubility, selectivity, bioavailability and metabolic stability [ 15 , 16 ]. In addition, bioisosteric replacement of hydrogen by fluorine in position 4 from the phenyl ring makes electronic modulation to reinforce and enhance the binding interaction process [ 12 , 17 ].…”

Section: Introductionmentioning

confidence: 99%

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Design, Synthesis, Cytotoxic Evaluation and Molecular Docking of New Fluoroquinazolinones as Potent Anticancer Agents with Dual EGFR Kinase and Tubulin Polymerization Inhibitory Effects

Zayed

Ahmed

Ihmaid

et al. 2018

IJMS

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A series of new fluoroquinazolinone 6–8 and 10a–g derivatives was designed, prepared and screened for their in vitro cytotoxic activity against human cancer cell lines MCF-7 and MDA-MBA-231. Compounds 6 (IC50 = 0.35 ± 0.01 µM), 10f (IC50 = 0.71 ± 0.01 µM), 10d (IC50 = 0.89 ± 0.02 µM) and 10a (IC50 = 0.95 ± 0.01 µM) displayed broad spectrum anticancer activity better than the reference drug gefitinib (IC50 = 0.97 ± 0.02 µM) against MCF-7. Compounds 10e (IC50 = 0.28 ± 0.02 µM), 10d (IC50 = 0.38 ± 0.01 µM), 7 (IC50 = 0.94 ± 0.07 µM) and 10c (IC50 = 1.09 ± 0.01 µM) showed better activity than the reference gefitinib (IC50 = 1.30 ± 0.04 µM) against MDA-MBA-231. Moreover, EGFR and tubulin inhibition assays were performed for the highest active derivatives and showed remarkable results comparing to the reference drugs. In order to assess and explain their binding affinities, molecular docking simulation was studied against EGFR and tubulin binding sites. The results obtained from molecular docking study and those obtained from cytotoxic screening were correlated.

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Section: Resultsmentioning

confidence: 99%

Section: Methodsmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

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Design, Synthesis, Cytotoxic Evaluation and Molecular Docking of New Fluoroquinazolinones as Potent Anticancer Agents with Dual EGFR Kinase and Tubulin Polymerization Inhibitory Effects

Zayed

Ahmed

Ihmaid

et al. 2018

IJMS

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“…DC. Leaves (Asteraceae) [ 125 ]. The study of endophytic fungus Annulohypoxylon stygium (Xylariaceae family) isolated from Bostrychia radicans algae led to the isolation of a novel compound, 3-benzylidene-2-methylhexahydropyrrolo [1,2-α] pyrazine-1,4-dione 390 ( Figure 12 ) [ 126 ].…”

Section: New Metabolites Isolated From Plant Endophytesmentioning

confidence: 99%

Biological Activities of Some New Secondary Metabolites Isolated from Endophytic Fungi: A Review Study

Zheng

Zhang

et al. 2021

IJMS

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Secondary metabolites isolated from plant endophytic fungi have been getting more and more attention. Some secondary metabolites exhibit high biological activities, hence, they have potential to be used for promising lead compounds in drug discovery. In this review, a total of 134 journal articles (from 2017 to 2019) were reviewed and the chemical structures of 449 new metabolites, including polyketides, terpenoids, steroids and so on, were summarized. Besides, various biological activities and structure-activity relationship of some compounds were aslo described.

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Exploration of Potent Cytotoxic Molecules from Fungi in Recent Past to Discover Plausible Anticancer Scaffolds

Shevkar

Pradhan

Armarkar

et al. 2022

Chemistry & Biodiversity

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Fungi are known to produce diverse scaffolds possessing unique biological activities, however, to date, no molecule discovered from a fungal source has reached the market as an anti‐cancer drug. Every year number of cytotoxic molecules of fungal origin are getting published and critical analysis of those compounds is necessary to identify the potent ones. A review mentioning the best cytotoxic fungal metabolites and their status in the drug development was published in 2014. In this report, we have included 176 cytotoxic molecules isolated from fungi after 2014 and categorized them according to their potencies such as IC50 values below 1 μM, 1–5 μM, and 5–10 μM. The emphasis was given to those 42 molecules which have shown IC50 less than 1 μM and discussed to a great extent. This review shall provide potent scaffolds of fungal origin which can be given priority in the development as a drug candidate for cancer therapeutics.

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Fusarithioamide B, a new benzamide derivative from the endophytic fungus Fusarium chlamydosporium with potent cytotoxic and antimicrobial activities

Cited by 58 publications

References 22 publications

Design, Synthesis, Cytotoxic Evaluation and Molecular Docking of New Fluoroquinazolinones as Potent Anticancer Agents with Dual EGFR Kinase and Tubulin Polymerization Inhibitory Effects

Design, Synthesis, Cytotoxic Evaluation and Molecular Docking of New Fluoroquinazolinones as Potent Anticancer Agents with Dual EGFR Kinase and Tubulin Polymerization Inhibitory Effects

Biological Activities of Some New Secondary Metabolites Isolated from Endophytic Fungi: A Review Study

Exploration of Potent Cytotoxic Molecules from Fungi in Recent Past to Discover Plausible Anticancer Scaffolds

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