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Acta Pharmaceutica, Vol. 61 No. 4, 2011.

Original scientific paper

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

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

MOSTAFA M. GHORAB ; Medicinal, Aromatic and Poisonous Plants Research Center (MAPPRC), College of Pharmacy, King Saud University, Riyadh, Saudi Arabia; Department of Drug Radiation Research, National Center for Radiation Research and Technology, PO Box 29, Nasr City, Cairo,
FATMA A. RAGAB ; Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Cairo University, Cairo, Egypt
HELMY I. HEIBA ; Department of Drug Radiation Research, National Center for Radiation Research and Technology, PO Box 29, Nasr City, Cairo, Egypt
MARWA G. EL-GAZZAR ; Department of Drug Radiation Research, National Center for Radiation Research and Technology, PO Box 29, Nasr City, Cairo, Egypt
MOSTAFA G. EL-GAZZAR ; Department of Drug Radiation Research, National Center for Radiation Research and Technology, PO Box 29, Nasr City, Cairo, Egypt

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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 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

Hrčak ID:

71386

URI

https://hrcak.srce.hr/71386

Publication date:

31.12.2011.

Article data in other languages: croatian

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