Login / Signup

Synthesis of cinnamils and quinoxalines and their biological evaluation as anticancer agents.

Ruei-Yu WangCai-Wei LiShu-Tse ChoChun-Hao ChangJih-Jung ChenTzenge-Lien Shih
Published in: Archiv der Pharmazie (2022)
We synthesized multiple cinnamils and quinoxalines to evaluate their anticancer activity. Cinnamils were used as precursors for quinoxalines via condensation with 1,2-diaminobenzene. Among the 26 synthesized compounds reported in this article, we found that cinnamil 3l exhibited its inhibitory effect with an IC 50 value of 1.45 ± 0.98 μM, significantly higher than doxorubicin (8.5 ± 0.85 μM) against pancreatic cancer cells (PANC-1). Additionally, cinnamil 3l (IC 50 10.98 ± 3.63 μM) showed less cytotoxicity than doxorubicin to Hs68 cells (0.92 ± 1.11 μM). The colony formation assay demonstrated that 3l obviously decreased the PANC-1 cell viability, and Western blot assays confirmed that 3l markedly induced apoptosis of PANC-1 cells through Bax, Bcl-2, and caspase 3 signaling cascades. These results demonstrate that cinnamil 3l has great potential to be further developed as a promising chemotherapeutic agent for pancreatic cancer.
Keyphrases
  • induced apoptosis
  • endoplasmic reticulum stress
  • signaling pathway
  • oxidative stress
  • drug delivery
  • high throughput
  • south africa
  • pi k akt
  • cell proliferation
  • risk assessment