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.
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Authors | Mohammad M Al-Sanea, Ghada H Al-Ansary, Zainab M Elsayed, Raed M Maklad, Eslam B Elkaeed, Mohamed A Abdelgawad, Syed Nasir Abbas Bukhari, Marwa M Abdel-Aziz, Howayda Suliman, Wagdy M Eldehna |
Journal | Journal of enzyme inhibition and medicinal chemistry
(J Enzyme Inhib Med Chem)
Vol. 36
Issue 1
Pg. 987-999
(Dec 2021)
ISSN: 1475-6374 [Electronic] England |
PMID | 33985397
(Publication Type: Journal Article)
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Chemical References |
- Antineoplastic Agents
- Benzofurans
- benzofuran
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Topics |
- Antineoplastic Agents
(chemical synthesis, chemistry, pharmacology)
- Apoptosis
(drug effects)
- Benzofurans
(chemical synthesis, chemistry, pharmacology)
- Carcinoma, Non-Small-Cell Lung
(drug therapy, metabolism, pathology)
- Cell Cycle
(drug effects)
- Cell Line, Tumor
- Cell Proliferation
(drug effects)
- Cell Survival
(drug effects)
- Dose-Response Relationship, Drug
- Drug Development
- Drug Screening Assays, Antitumor
- Humans
- Lung Neoplasms
(drug therapy, metabolism, pathology)
- Molecular Structure
- Structure-Activity Relationship
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