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Synthesis and biological evaluation of 1-(benzofuran-3-yl)-4-(3,4,5-trimethoxyphenyl)-1H-1,2,3-triazole derivatives as tubulin polymerization inhibitors. | LitMetric

AI Article Synopsis

  • Microtubules and the mitotic spindle play crucial roles in cell division, making them potential targets for cancer treatment.
  • A compound named 6-Methoxy-N-phenyl-3-(4-(3,4,5-trimethoxyphenyl)-1H-1,2,3-triazol-1-yl)benzofuran-2-carboxamide (17g) showed strong anti-cancer activity against various cancer cell lines with IC values between 0.57 and 5.7 μM.
  • Mechanistic studies suggest that 17g works by inhibiting tubulin polymerization, disrupting mitotic spindle formation, causing cell cycle arrest in the G2/M phase, and leading to cell

Article Abstract

The key functions of microtubules and the mitotic spindle in cell division make them attractive targets for cancer therapy. In this study, a series of 1-(benzofuran-3-yl)-4-(3,4,5-trimethoxyphenyl)-1H-1,2,3-triazole derivatives was synthesized, and their antiproliferative activities against HCT116, HeLa, HepG2, and A549 cells were evaluated. 6-Methoxy-N-phenyl-3-(4-(3,4,5-trimethoxyphenyl)-1H-1,2,3-triazol-1-yl)benzofuran-2-carboxamide (17g) exhibited the strongest antiproliferative activities, with IC values ranging from 0.57 to 5.7 μM. Mechanistic studies showed that 17g inhibited tubulin polymerization, leading to the disruption of mitotic spindle formation, cell cycle arrest in the G2/M phase, and apoptosis of A549 cells. A docking study indicated that 17g was a good molecular fit at the colchicine binding site of tubulin. These results showed that 17g is a potential anticancer compound that is worthy of further development as a tubulin polymerization inhibitor.

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http://dx.doi.org/10.1016/j.bioorg.2019.103392DOI Listing

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