Acta Pharm. 61 (2011) 415-425

 

full paper

Original research paper

 

Synthesis, in vitro anticancer screening and radiosensitizing evaluation of some new 4-[3-(substituted)thioureido]-N-(quinoxalin-2-yl)benzenesulfonamide derivatives

MOSTAFA M.GHORAB, FATMA A. RAGAB, HELMY I. HEIBA, MARWA G. EL-GAZZAR and MOSTAFA G. EL-GAZZAR

marwagalalgazzar@yahoo.com

1 Medicinal, Aromatic and Poisonous Plants Research Center (MAPPRC), College of Pharmacy, King Saud University, Riyadh, Saudi Arabia

2 Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Cairo University, Cairo, Egypt

3 Department of Drug Radiation Research, National Center for Radiation Research and Technology, PO Box 29, Nasr City, Cairo, Egypt

Accepted December 1, 2011

 

Sulfonamides and quinoxaline derivatives possess many types of biological activities and have been recently reported to show substantial antitumor activity. This paper reports the synthesis of novel thioureidosulfaquinoxaline derivatives. All the newly synthesized compounds were evaluated for their in vitro anticancer activity against a human liver cell line (HEPG2) and showed higher activity than the reference drug doxorubicin. 4-(3-(4-Ethylbenzoate)thioureido)-N-(quinoxalin-2-yl)benzenesulfonamide (9) (IC50 = 15.6 µmol L-1), N-(pyridin-2-yl)-4-(3-(4-(N-quinoxalin-2-yl-sulfamoyl)phenyl)thioureido)benzene-sulfonamide (10) (IC50 = 26.8 µmol L-1) and N-(quinoxalin-2-yl)-4-(3-(4-(N-thiazol-2-ylsulfamoyl)phenyl)thioureido)benzenesulfonamide (11) (IC50 = 24.4 µmol L-1) were the most potent compared to doxorubicin (IC50 = 71.8 µmol L-1). The most potent compounds 9, 10 and 11 were evaluated as radiosensitizing agents by subjecting the compounds to γ-irradiation (8 kGy).

 

Keywords: quinoxaline, sulfonamide, anticancer activity, radiosensitizing effect