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

Abstract

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.

Synthesis of selenophene‐based chalcone analogs and assessment of their biological activity as anticancer agents

“…The clonogenic assay was performed using the reference method with a slight modification. [55] HT-29 cells were seeded in 6-well plates at 3500 cells per well and incubated for 24 h. Next, the cells were treated with the indicated concentrations of compounds 6 (5, 10, 20, and 40 μM), 5-FU (positive control, 40 μM), or vehicle (DMSO) and allowed to form colonies for 14 days. The colonies were washed thrice with PBS, and the cells attached to the plastic surface were fixed in 99% MeOH for 30 min.…”

“…Western blot analysis was performed according to a previously reported protocol. [55] Briefly, HT-29 cells (6 × 10 5 cells) were seeded into 6-cm dishes. After reaching 85%-90% confluence, different concentrations (5,10,20, and 40 μM) of compound 6 or 5-FU (positive control, 40 μM) were added.…”