A series of 27 differently substituted 4-anilinofuro]2,3-b]quinolines were synthesized and evaluated for their antiproliferative activities against the HeLa, SKHep1, SAS, AGS, A549, and CE81T cell lines, cancers commonly found in Asian countries. Among the compounds tested, 1-4-[(3-chloro-7-methoxyfure [2,3-b]quinolin-4-yl) amino]phenyl)ethanone (1) was the most potent, with IC50 values of 3.1,3.0, and 4.2 μm, resp., against the growth of HeLa, SKHep, and CE81T cells. Compound 1 was, thus, further evaluated by flow cytometry to evaluate its effect on the cell-cycle distribution of HeLa cells. Our results indicated that 1 readily induces cell-cycle arrest in the G2/M phase, followed by DNA fragmentation and, ultimately, cell death.
All Science Journal Classification (ASJC) codes
- Molecular Medicine
- Molecular Biology