Title:Synthesis of Novel Urea and Sulfonamide Derivatives of Isatin Schiff Bases
as Potential Anti-cancer Agents
Volume: 19
Issue: 9
Author(s): Ural U. Demirel, Süreyya Ölgen*, Ecem F. Karaman, Mehmet Tanol, Sibel Özden and Hakan Göker
Affiliation:
- Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Biruni University, Istanbul, Turkey
Keywords:
Urea and sulfonamide derivatives, isatin, schiff bases, cytotoxicity, ADME prediction, synthesis, molecular docking.
Abstract:
Background: Among the many types of chemical scaffolds, isatin derivatives, including their
Schiff bases, have been extensively studied to find novel therapeutic agents against cancer. Amide or urea
groups containing derivatives were also discovered to be tyrosine kinase inhibitors.
Objective: This study aims to find potent compounds by designing 16 novel urea and sulfonamide derivatives
of isatin Schiff bases.
Methods: Compounds were tested against PC-3, HepG2, SH-SY5Y, A549 cancerous, and NIH/3T3 noncancerous
cell lines using cell culture assay.
Results: Among the tested compounds 7a, 7b, 7c, 7d, 7h, 8a, and 8f presented potential inhibitions
against cellular proliferation activities of HepG2 cells with average IC50 values of 31.97, 42.13, 31.50,
47.98, 32.59, 43.44, and 37.81 μM, respectively. They showed better inhibition potencies than the reference
compound doxorubicin, and its value was measured as 51.15 μM in the same culture assay. The
cytotoxic activities of the compounds in other cell lines were found to be less potent compared to doxorubicin.
Conclusion: In vitro experiments demonstrated that designed compounds have the first evidence that they
might be active against hepatocellular carcinoma. According to ADME prediction results, all compounds
presented drug-like and good metabolic properties.
