A novel series of urea-linked ciprofloxacin (CP)-chalcone hybrids 3a-j were synthesized and screened by NCI-60
cancer cell lines as potential cytotoxic agents. Interestingly, compounds 3c and 3j showed remarkable antiproliferative
activities against both colon HCT-116 and leukemia SR cancer cells compared to camptothecin,
topotecan and staurosporine with IC50 = 2.53, 2.01, 17.36, 12.23 and 3.1 μM for HCT-116 cells, respectively and
IC50 = 0.73, 0.64, 3.32, 13.72 and 1.17 μM for leukemia SR cells, respectively. Also, compounds 3c and 3j
exhibited inhibitory activities against Topoisomerase (Topo) I with % inhibition = 51.19% and 56.72%,
respectively, compared to camptothecin (% inhibition = 60.05%) and Topo IIβ with % inhibition = 60.81% and
60.06%, respectively, compared to topotecan (% inhibition = 71.09%). Furthermore, compound 3j arrested the
cell cycle of leukemia SR cells at G2/M phase. It induced apoptosis both intrinsically and extrinsically via
activation of proteolytic caspases cascade (caspases-3,
Research Department
Research Journal
Bioorg, Chem.
Research Publisher
Elsevier
Research Rank
1
Research Vol
106
Research Website
https://www.sciencedirect.com/science/article/abs/pii/S004520682031720X
Research Year
2021
Research Member
Research Abstract