Anticancer and radio-sensitizing evaluation of some new sulfonamide derivatives bearing pyridone, thiophene, and hydrazone moieties

作者：Ghorab Mostafa M^*; Ragab Fatma A; Heiba Helmy I; Soliman Aiten M

来源：Research on Chemical Intermediates, 2017, 43(8): 4657-4681.

DOI：10.1007/s11164-017-2903-x

• Sulfonamide
• Pyridone
• Thiophene
• Hydrazone
• Anticancer
• Radiosensitizers

A series of new pyridone 5, 6, 8a-j, hydrazone 7a-j, and thiophene 9-12 derivatives bearing a sulfonamide moiety were synthesized from the starting material 4-chloro-N-(4-(1-(2-(2-cyanoacetyl)hydrazono)ethyl)phenyl) benzenesulfonamide 4. The target compounds were in vitro evaluated for their cytotoxic activity against a human liver cancer cell line (HepG2). Compounds 4 and 8d-j showed higher cytotoxic activity compared to doxorubicin, as a positive control. The radio-sensitizing ability of the promising compounds 4, 8d, and 8h was studied which showed an enhanced cytotoxic activity after combination with gamma-radiation. Molecular modeling was performed in CA II/IX mimic active site to predict the binding possibility of the target compounds. All the synthesized compounds showed appropriate fitting with the amino acids in the binding pocket on the basis of their S score data and binding interactions. This binding possibility might contribute at least in part, to their anticancer activity.

• 出版日期2017-8