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

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.
AuthorsMohammad 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
JournalJournal 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
PMID33985397 (Publication Type: Journal Article)
Chemical References
  • Antineoplastic Agents
  • Benzofurans
  • benzofuran
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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