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Development of 3-methyl/3-(morpholinomethyl)benzofuran derivatives as novel antitumor agents towards non-small cell lung cancer cells.
- Source :
-
Journal of enzyme inhibition and medicinal chemistry [J Enzyme Inhib Med Chem] 2021 Dec; Vol. 36 (1), pp. 987-999. - Publication Year :
- 2021
-
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 IC <subscript>50</subscript> 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 IC <subscript>50</subscript> equal 77.97, 132.5 and 45.4 nM, respectively.
- Subjects :
- Antineoplastic Agents chemical synthesis
Antineoplastic Agents chemistry
Apoptosis drug effects
Benzofurans chemical synthesis
Benzofurans chemistry
Carcinoma, Non-Small-Cell Lung metabolism
Carcinoma, Non-Small-Cell Lung pathology
Cell Cycle drug effects
Cell Line, Tumor
Cell Proliferation drug effects
Cell Survival drug effects
Dose-Response Relationship, Drug
Drug Screening Assays, Antitumor
Humans
Lung Neoplasms metabolism
Lung Neoplasms pathology
Molecular Structure
Structure-Activity Relationship
Antineoplastic Agents pharmacology
Benzofurans pharmacology
Carcinoma, Non-Small-Cell Lung drug therapy
Drug Development
Lung Neoplasms drug therapy
Subjects
Details
- Language :
- English
- ISSN :
- 1475-6374
- Volume :
- 36
- Issue :
- 1
- Database :
- MEDLINE
- Journal :
- Journal of enzyme inhibition and medicinal chemistry
- Publication Type :
- Academic Journal
- Accession number :
- 33985397
- Full Text :
- https://doi.org/10.1080/14756366.2021.1915302