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Arzneimittelforschung 2012; 62(01): 46-52
DOI: 10.1055/s-0031-1295496
Original Article
© Georg Thieme Verlag KG Stuttgart · New York

Synthesis, in-vitro Anticancer Screening and Radiosensitizing Evaluation of some New N-(quinoxalin-2-yl)benzenesulfonamide Derivatives

M. M. Ghorab
1   Department of Drug Radiation Research, National Center for Radiation Research and Technology (NCRRT), Atomic Energy Authority, Cairo, Egypt
3   Medicinal, Aromatic and Poisonous Plants Research Center (MAPPRC), College of Pharmacy, King Saud University, Riyadh, Saudi Arabia
,
F. A. Ragab
2   Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Cairo University, Cairo, Egypt
,
H. I. Heiba
1   Department of Drug Radiation Research, National Center for Radiation Research and Technology (NCRRT), Atomic Energy Authority, Cairo, Egypt
,
M. G. El-Gazzar
1   Department of Drug Radiation Research, National Center for Radiation Research and Technology (NCRRT), Atomic Energy Authority, Cairo, Egypt
,
M. G. El-Gazzar
1   Department of Drug Radiation Research, National Center for Radiation Research and Technology (NCRRT), Atomic Energy Authority, Cairo, Egypt
› Author Affiliations
Further Information

Publication History

received 14 September 2011

accepted 17 October 2011

Publication Date:
10 January 2012 (online)

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Abstract

The objective of this work is to synthesize and investigate the anticancer activity of a new series of sulfaquinoxaline derivatives by incorporating biologically active moieties (thiourethane, thiazole, imidazole, imidazopyrimidine, imidazopyrimido-pyrimidine, thienopyrimidine, benzopyrimidinone, benzothiazole, thiazole and pyridine moieties). All the newly synthesized compounds were evaluated for their in-vitro anticancer activity against human liver cell line (HEPG2). All the tested compounds showed comparable activity to that of the reference drug 5-fluorouracil (IC50=40 µM), and the most potent compounds were found to be compounds 4 and 17 (IC50=4.29 and 11.27 µM, respectively). On the other hand, the most potent compounds 4 and 17 were evaluated as radiosensitizing agents.

Key words

sulfonamide - quinoxaline - anticancer - radiosensitizing
 

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