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-(morpholi...
| Main Authors: | , , , , , , , , , |
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| Format: | Article |
| Language: | English |
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Taylor & Francis Group
2021-01-01
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| Series: | Journal of Enzyme Inhibition and Medicinal Chemistry |
| Subjects: | |
| Online Access: | http://dx.doi.org/10.1080/14756366.2021.1915302 |
| _version_ | 1798016054801203200 |
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| author | 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 |
| author_facet | 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 |
| author_sort | Mohammad M. Al-Sanea |
| collection | DOAJ |
| description | 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. |
| first_indexed | 2024-04-11T15:44:35Z |
| format | Article |
| id | doaj.art-4937eac42cac423d896bc874b19c1198 |
| institution | Directory Open Access Journal |
| issn | 1475-6366 1475-6374 |
| language | English |
| last_indexed | 2024-04-11T15:44:35Z |
| publishDate | 2021-01-01 |
| publisher | Taylor & Francis Group |
| record_format | Article |
| series | Journal of Enzyme Inhibition and Medicinal Chemistry |
| spelling | doaj.art-4937eac42cac423d896bc874b19c11982022-12-22T04:15:37ZengTaylor & Francis GroupJournal of Enzyme Inhibition and Medicinal Chemistry1475-63661475-63742021-01-0136198799910.1080/14756366.2021.19153021915302Development of 3-methyl/3-(morpholinomethyl)benzofuran derivatives as novel antitumor agents towards non-small cell lung cancer cellsMohammad M. Al-Sanea0Ghada H. Al-Ansary1Zainab M. Elsayed2Raed M. Maklad3Eslam B. Elkaeed4Mohamed A. Abdelgawad5Syed Nasir Abbas Bukhari6Marwa M. Abdel-Aziz7Howayda Suliman8Wagdy M. Eldehna9Department of Pharmaceutical Chemistry, College of Pharmacy, Jouf UniversityDepartment of Pharmaceutical Chemistry, Pharmacy Program, Batterejee Medical CollegeScientific Research and Innovation Support Unit, Faculty of Pharmacy, Kafrelsheikh UniversityDepartment of Pharmaceutical Chemistry, Faculty of Pharmacy, Kafrelsheikh UniversityDepartment of Pharmaceutical Sciences, College of Pharmacy, AlMaarefa UniversityDepartment of Pharmaceutical Chemistry, College of Pharmacy, Jouf UniversityDepartment of Pharmaceutical Chemistry, College of Pharmacy, Jouf UniversityThe Regional Center for Mycology & Biotechnology, Al-Azhar UniversityDepartment of Medical Biochemistry, Faculty of Medicine, Alexandria UniversityDepartment of Pharmaceutical Chemistry, Faculty of Pharmacy, Kafrelsheikh UniversityAs 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.http://dx.doi.org/10.1080/14756366.2021.1915302benzofuran-2-carbohydrazideanticancer agentslung cancervegfr-2 inhibitors |
| spellingShingle | 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 Development of 3-methyl/3-(morpholinomethyl)benzofuran derivatives as novel antitumor agents towards non-small cell lung cancer cells Journal of Enzyme Inhibition and Medicinal Chemistry benzofuran-2-carbohydrazide anticancer agents lung cancer vegfr-2 inhibitors |
| title | Development of 3-methyl/3-(morpholinomethyl)benzofuran derivatives as novel antitumor agents towards non-small cell lung cancer cells |
| title_full | Development of 3-methyl/3-(morpholinomethyl)benzofuran derivatives as novel antitumor agents towards non-small cell lung cancer cells |
| title_fullStr | Development of 3-methyl/3-(morpholinomethyl)benzofuran derivatives as novel antitumor agents towards non-small cell lung cancer cells |
| title_full_unstemmed | Development of 3-methyl/3-(morpholinomethyl)benzofuran derivatives as novel antitumor agents towards non-small cell lung cancer cells |
| title_short | Development of 3-methyl/3-(morpholinomethyl)benzofuran derivatives as novel antitumor agents towards non-small cell lung cancer cells |
| title_sort | development of 3 methyl 3 morpholinomethyl benzofuran derivatives as novel antitumor agents towards non small cell lung cancer cells |
| topic | benzofuran-2-carbohydrazide anticancer agents lung cancer vegfr-2 inhibitors |
| url | http://dx.doi.org/10.1080/14756366.2021.1915302 |
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