Synthesis and antitumor evaluation of some novel sulfonamide derivatives with studying their potential synergistic effect with Þ-irradiation / Aiten Mahmoud Mohamed Mohamed Soliman ; Supervised Fatma Abdelfattah Ragab , Helmy Ismail Heiba

Thesis (Ph.D.) - Cairo University - Faculty of Pharmacy - Department of Pharmaceutical Chemistry

The present work reports the synthesis of some new sulfonamide derivatives containing hydrazone, thiophene and pyridone moieties. Forty three new compounds were synthesized. All the newly synthesized compounds were identified on the basis of elemental analysis and spectroscopic methods, then subjected to in vitro cytotoxic screening against human hepatocellular liver carcinoma cell line (HepG2). Most of the newly synthesized compounds showed better cytotoxic activity when compared to the reference drug, doxorubicin. Some of the most potent compounds were selected to be evaluated again for their in vitro cytotoxic activity in combination with Þ-radiation and showed interesting radiosensitizing activity. The newly synthesized compounds were docked inside the active site of hCA IX (human carbonic anhydrase IX) in an attempt to predict their anticancer mechanism of action. All the compounds showed appropriate fitting with the relevant amino acids in the binding pocket on the basis of standard bond lengths, angles, S score and E conformation data

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