{
"id": "https://doi.org/10.6084/m9.figshare.20509718",
"doi": "10.6084/M9.FIGSHARE.20509718",
"url": "https://tandf.figshare.com/articles/journal_contribution/Anti-cancer_and_immunomodulatory_evaluation_of_new_nicotinamide_derivatives_as_potential_VEGFR-2_inhibitors_and_apoptosis_inducers_i_in_vitro_i_and_i_in_silico_i_studies/20509718",
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"creators": [
{
"name": "Yousef, Reda G.",
"givenName": "Reda G.",
"familyName": "Yousef"
},
{
"name": "Elwan, Alaa",
"givenName": "Alaa",
"familyName": "Elwan"
},
{
"name": "Gobaara, Ibraheem M. M.",
"givenName": "Ibraheem M. M.",
"familyName": "Gobaara"
},
{
"name": "Mehany, Ahmed B. M.",
"givenName": "Ahmed B. M.",
"familyName": "Mehany"
},
{
"name": "Eldehna, Wagdy M.",
"givenName": "Wagdy M.",
"familyName": "Eldehna"
},
{
"name": "El-Metwally, Souad A.",
"givenName": "Souad A.",
"familyName": "El-Metwally"
},
{
"name": "Alsfouk, Bshra A.",
"givenName": "Bshra A.",
"familyName": "Alsfouk"
},
{
"name": "Elkaeed, Eslam B.",
"givenName": "Eslam B.",
"familyName": "Elkaeed"
},
{
"name": "Metwaly, Ahmed M.",
"givenName": "Ahmed M.",
"familyName": "Metwaly"
},
{
"name": "Eissa, Ibrahim H.",
"givenName": "Ibrahim H.",
"familyName": "Eissa"
}
],
"titles": [
{
"title": "Anti-cancer and immunomodulatory evaluation of new nicotinamide derivatives as potential VEGFR-2 inhibitors and apoptosis inducers: in vitro and in silico studies"
}
],
"publisher": {
"name": "Taylor & Francis"
},
"container": {},
"subjects": [
{
"subject": "Biochemistry"
},
{
"subject": "Medicine"
},
{
"subject": "Cell Biology"
},
{
"subject": "Pharmacology"
},
{
"subject": "Environmental Sciences not elsewhere classified"
},
{
"subject": "Chemical Sciences not elsewhere classified"
},
{
"subject": "Biological Sciences not elsewhere classified"
},
{
"subject": "Information Systems not elsewhere classified"
},
{
"subject": "Cancer"
},
{
"subject": "Hematology"
}
],
"contributors": [],
"dates": [
{
"date": "2022-08-18",
"dateType": "Created"
},
{
"date": "2024-03-21",
"dateType": "Updated"
},
{
"date": "2022",
"dateType": "Issued"
}
],
"publicationYear": 2022,
"identifiers": [],
"sizes": [
"2384826 Bytes"
],
"formats": [],
"rightsList": [
{
"rights": "Creative Commons Attribution 4.0 International",
"rightsUri": "https://creativecommons.org/licenses/by/4.0/legalcode",
"schemeUri": "https://spdx.org/licenses/",
"rightsIdentifier": "cc-by-4.0",
"rightsIdentifierScheme": "SPDX"
}
],
"descriptions": [
{
"description": "New nicotinamide derivatives 6, 7, 10, and 11 were designed and synthesised based on the essential features of the VEGFR-2 inhibitors. Compound 10 revealed the highest anti-proliferative activities with IC50 values of 15.4 and 9.8 µM against HCT-116 and HepG2, respectively compared to sorafenib (IC50 = 9.30 and 7.40 µM). Compound 7 owned promising cytotoxic activities with IC50 values of 15.7 and 15.5 µM against the same cell lines, respectively. Subsequently, the VEGFR-2 inhibitory activities were assessed for the titled compounds to exhibit VEGFR-2 inhibition with sub-micromolar IC50 values. Moreover, compound 7 induced the cell cycle cessation at the cycle at %G2-M and G0-G1phases, and induced apoptosis in the HCT-116. Compounds 7 and 10 reduced the levels of TNF-α by 81.6 and 84.5% as well as IL-6 by 88.4 and 60.9%, respectively, compared to dexamethasone (82.4 and 93.1%). In silico docking, molecular dynamics simulations, ADMET, and toxicity studies were carried out.",
"descriptionType": "Abstract"
}
],
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"relatedIdentifiers": [
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"relationType": "IsSupplementTo",
"relatedIdentifier": "10.1080/14756366.2022.2110868",
"relatedIdentifierType": "DOI"
}
],
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