Development of 3-methyl/3-(morpholinomethyl)benzofuran derivatives as novel antitumor agents towards non-small cell lung cancer cells.

Al-Sanea, MM; Al-Ansary, GH; Elsayed, ZM; Maklad, RM; Elkaeed, EB; Abdelgawad, MA; Bukhari, SNA; Abdel-Aziz, MM; Suliman, H; Eldehna, WM

Development of 3-methyl/3-(morpholinomethyl)benzofuran derivatives as novel antitumor agents towards non-small cell lung cancer cells.

Al-Sanea, MM Al-Ansary, GH Elsayed, ZM Maklad, RM Elkaeed, EB Abdelgawad, MA Bukhari, SNA Abdel-Aziz, MM Suliman, H Eldehna, WM

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Publisher:: TAYLOR & FRANCIS LTD
Publication Type:: Journal Article
Citation:: J Enzyme Inhib Med Chem, 2021, 36, (1), pp. 987-999
Issue Date:: 2021-12

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Field	Value	Language
dc.contributor.author	Al-Sanea, MM
dc.contributor.author	Al-Ansary, GH
dc.contributor.author	Elsayed, ZM
dc.contributor.author	Maklad, RM
dc.contributor.author	Elkaeed, EB
dc.contributor.author	Abdelgawad, MA
dc.contributor.author	Bukhari, SNA
dc.contributor.author	Abdel-Aziz, MM
dc.contributor.author	Suliman, H
dc.contributor.author	Eldehna, WM
dc.date.accessioned	2025-01-31T01:21:39Z
dc.date.available	2025-01-31T01:21:39Z
dc.date.issued	2021-12
dc.identifier.citation	J Enzyme Inhib Med Chem, 2021, 36, (1), pp. 987-999
dc.identifier.issn	1475-6366
dc.identifier.issn	1475-6374
dc.identifier.uri	http://hdl.handle.net/10453/184737
dc.description.abstract	As one of the most lethal malignancies, lung cancer is considered to account for approximately one-fifth of all malignant tumours-related deaths worldwide. This study reports the synthesis and in vitro biological assessment of two sets of 3-methylbenzofurans (4a-d, 6a-c, 8a-c and 11) and 3-(morpholinomethyl)benzofurans (15a-c, 16a-b, 17a-b and 18) as potential anticancer agents towards non-small cell lung carcinoma A549 and NCI-H23 cell lines, with VEGFR-2 inhibitory activity. The target benzofuran-based derivatives efficiently inhibited the growth of both A549 and NCI-H23 cell lines with IC50 spanning in ranges 1.48-47.02 and 0.49-68.9 µM, respectively. The three most active benzofurans (4b, 15a and 16a) were further investigated for their effects on the cell cycle progression and apoptosis in A549 (for 4b) and NCI-H23 (for 15a and 16a) cell lines. Furthermore, benzofurans 4b, 15a and 16a displayed good VEGFR-2 inhibitory activity with IC50 equal 77.97, 132.5 and 45.4 nM, respectively.
dc.format	Print
dc.language	eng
dc.publisher	TAYLOR & FRANCIS LTD
dc.relation.ispartof	J Enzyme Inhib Med Chem
dc.relation.isbasedon	10.1080/14756366.2021.1915302
dc.rights	info:eu-repo/semantics/openAccess
dc.subject	0304 Medicinal and Biomolecular Chemistry, 0601 Biochemistry and Cell Biology
dc.subject.classification	Medicinal & Biomolecular Chemistry
dc.subject.classification	3404 Medicinal and biomolecular chemistry
dc.subject.mesh	Antineoplastic Agents
dc.subject.mesh	Apoptosis
dc.subject.mesh	Benzofurans
dc.subject.mesh	Carcinoma, Non-Small-Cell Lung
dc.subject.mesh	Cell Cycle
dc.subject.mesh	Cell Line, Tumor
dc.subject.mesh	Cell Proliferation
dc.subject.mesh	Cell Survival
dc.subject.mesh	Dose-Response Relationship, Drug
dc.subject.mesh	Drug Development
dc.subject.mesh	Drug Screening Assays, Antitumor
dc.subject.mesh	Humans
dc.subject.mesh	Lung Neoplasms
dc.subject.mesh	Molecular Structure
dc.subject.mesh	Structure-Activity Relationship
dc.subject.mesh	Cell Line, Tumor
dc.subject.mesh	Humans
dc.subject.mesh	Carcinoma, Non-Small-Cell Lung
dc.subject.mesh	Lung Neoplasms
dc.subject.mesh	Benzofurans
dc.subject.mesh	Antineoplastic Agents
dc.subject.mesh	Drug Screening Assays, Antitumor
dc.subject.mesh	Cell Cycle
dc.subject.mesh	Apoptosis
dc.subject.mesh	Cell Proliferation
dc.subject.mesh	Cell Survival
dc.subject.mesh	Molecular Structure
dc.subject.mesh	Structure-Activity Relationship
dc.subject.mesh	Dose-Response Relationship, Drug
dc.subject.mesh	Drug Development
dc.subject.mesh	Antineoplastic Agents
dc.subject.mesh	Apoptosis
dc.subject.mesh	Benzofurans
dc.subject.mesh	Carcinoma, Non-Small-Cell Lung
dc.subject.mesh	Cell Cycle
dc.subject.mesh	Cell Line, Tumor
dc.subject.mesh	Cell Proliferation
dc.subject.mesh	Cell Survival
dc.subject.mesh	Dose-Response Relationship, Drug
dc.subject.mesh	Drug Development
dc.subject.mesh	Drug Screening Assays, Antitumor
dc.subject.mesh	Humans
dc.subject.mesh	Lung Neoplasms
dc.subject.mesh	Molecular Structure
dc.subject.mesh	Structure-Activity Relationship
dc.title	Development of 3-methyl/3-(morpholinomethyl)benzofuran derivatives as novel antitumor agents towards non-small cell lung cancer cells.
dc.type	Journal Article
utslib.citation.volume	36
utslib.location.activity	England
utslib.for	0304 Medicinal and Biomolecular Chemistry
utslib.for	0601 Biochemistry and Cell Biology
pubs.organisational-group	University of Technology Sydney
pubs.organisational-group	University of Technology Sydney/Faculty of Science
pubs.organisational-group	University of Technology Sydney/Faculty of Science/School of Mathematical and Physical Sciences
utslib.copyright.status	open_access	*
dc.rights.license	This work is licensed under a Creative Commons Attribution 4.0 International License (CC BY 4.0). To view a copy of this license, visit https://creativecommons.org/licenses/by/4.0/
dc.date.updated	2025-01-31T01:21:36Z
pubs.issue	1
pubs.publication-status	Published
pubs.volume	36
utslib.citation.issue	1

Abstract:

As one of the most lethal malignancies, lung cancer is considered to account for approximately one-fifth of all malignant tumours-related deaths worldwide. This study reports the synthesis and in vitro biological assessment of two sets of 3-methylbenzofurans (4a-d, 6a-c, 8a-c and 11) and 3-(morpholinomethyl)benzofurans (15a-c, 16a-b, 17a-b and 18) as potential anticancer agents towards non-small cell lung carcinoma A549 and NCI-H23 cell lines, with VEGFR-2 inhibitory activity. The target benzofuran-based derivatives efficiently inhibited the growth of both A549 and NCI-H23 cell lines with IC50 spanning in ranges 1.48-47.02 and 0.49-68.9 µM, respectively. The three most active benzofurans (4b, 15a and 16a) were further investigated for their effects on the cell cycle progression and apoptosis in A549 (for 4b) and NCI-H23 (for 15a and 16a) cell lines. Furthermore, benzofurans 4b, 15a and 16a displayed good VEGFR-2 inhibitory activity with IC50 equal 77.97, 132.5 and 45.4 nM, respectively.

Please use this identifier to cite or link to this item:

http://hdl.handle.net/10453/184737