开发 3-甲基/3-(吗啉甲基)苯并呋喃衍生物作为新型抗肿瘤剂用于治疗非小细胞肺癌细胞。

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

机构信息

Department of Pharmaceutical Chemistry, College of Pharmacy, Jouf University, Sakaka, Saudi Arabia.

Department of Pharmaceutical Chemistry, Pharmacy Program, Batterejee Medical College, Jeddah, Saudi Arabia.

出版信息

J Enzyme Inhib Med Chem. 2021 Dec;36(1):987-999. doi: 10.1080/14756366.2021.1915302.

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 biological assessment of two sets of 3-methylbenzofurans (, , and ) and 3-(morpholinomethyl)benzofurans (, , and ) 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 spanning in ranges 1.48-47.02 and 0.49-68.9 µM, respectively. The three most active benzofurans (, and ) were further investigated for their effects on the cell cycle progression and apoptosis in A549 (for ) and NCI-H23 (for and ) cell lines. Furthermore, benzofurans , and displayed good VEGFR-2 inhibitory activity with IC equal 77.97, 132.5 and 45.4 nM, respectively.

作为最致命的恶性肿瘤之一，肺癌被认为占全球所有恶性肿瘤相关死亡人数的五分之一左右。本研究报告了两组 3-甲基苯并呋喃（、、和）和 3-（吗啉甲基）苯并呋喃（、、和）的合成和生物评估，它们作为潜在的抗癌剂，针对非小细胞肺癌 A549 和 NCI-H23 细胞系，具有 VEGFR-2 抑制活性。基于苯并呋喃的目标衍生物有效地抑制了 A549 和 NCI-H23 细胞系的生长，IC 范围分别为 1.48-47.02 和 0.49-68.9 μM。进一步研究了三种最活跃的苯并呋喃（、和）对 A549（用于）和 NCI-H23（用于和）细胞系细胞周期进展和凋亡的影响。此外，苯并呋喃、和显示出良好的 VEGFR-2 抑制活性，IC 分别为 77.97、132.5 和 45.4 nM。