<abstract xml:lang="en" xmlns="http://www.w3.org/1999/xhtml">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 thioureido sulfaquinoxaline derivatives. All the newly synthesized compounds were evaluated for their <italic>in vitro</italic> anticancer activity against a human liver cell line (HEPG2) and showed higher activity than the reference drug doxorubicin. 4-(3-(4-Ethylbenzoate) thioureido)-<italic>N</italic>-(quinoxalin-2-yl)benzenesulfonamide (<bold>9</bold>) (<italic>IC</italic>50 = 15.6 μmol L-1), <italic>N</italic>-(pyridin-2-yl)-4-(3-(4-(<italic>N</italic>-quinoxalin-2-yl-sulfamoyl)phenyl)thioureido)benzenesulfonamide (<bold>10</bold>) (<italic>IC</italic>50 = 26.8 μmol L-1) and <italic>N</italic>-(quinoxalin-2-yl)-4-(3-(4-(<italic>N</italic>-thiazol-2-ylsulfamoyl)phenyl)thioureido)benzenesulfonamide (<bold>11</bold>) (<italic>IC</italic>50 = 24.4 μmol L-1) were the most potent compared to doxorubicin (<italic>IC</italic>50 = 71.8 μmol L-1). The most potent compounds <bold>9, 10</bold> and <bold>11</bold> were evaluated as radiosensitizing agents by subjecting the compounds to γ-irradiation (8 kGy).</abstract>

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 thioureido sulfaquinoxaline 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)benzenesulfonamide (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).

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

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

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

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

Acta Pharmaceutica

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

Sulfonamides and quinoxaline derivatives possess many types of biological activities and have been recently reported to show substantial antitumor activity....

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

Published Online: Dec 25, 2011

Page range: 415 - 425

DOI: https://doi.org/10.2478/v10007-011-0040-4

Keywords
kinoksalin, sulfonamid, antitumorsko djelovanje, radiosenzitirajući učinak

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