Development of 3-methyl/3-(morpholinomethyl)benzofuran derivatives as novel antitumor agents towards non-small cell lung cancer cells
Copyright policy )Development of 3-methyl/3-(morpholinomethyl)benzofuran derivatives as novel antitumor agents towards non-small cell lung cancer cells
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.
- Batterjee Medical College Saudi Arabia
- Beni-Suef University Egypt
- Ain Shams University Egypt
- Kafrelsheikh University Egypt
- Al Azhar University Egypt
Lung Neoplasms, Cell Survival, Antineoplastic Agents, Apoptosis, RM1-950, anticancer agents, Structure-Activity Relationship, Drug Development, Carcinoma, Non-Small-Cell Lung, Cell Line, Tumor, Humans, benzofuran-2-carbohydrazide, Benzofurans, Cell Proliferation, Dose-Response Relationship, Drug, Molecular Structure, Cell Cycle, lung cancer, Therapeutics. Pharmacology, Drug Screening Assays, Antitumor, vegfr-2 inhibitors, Research Paper
Lung Neoplasms, Cell Survival, Antineoplastic Agents, Apoptosis, RM1-950, anticancer agents, Structure-Activity Relationship, Drug Development, Carcinoma, Non-Small-Cell Lung, Cell Line, Tumor, Humans, benzofuran-2-carbohydrazide, Benzofurans, Cell Proliferation, Dose-Response Relationship, Drug, Molecular Structure, Cell Cycle, lung cancer, Therapeutics. Pharmacology, Drug Screening Assays, Antitumor, vegfr-2 inhibitors, Research Paper
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