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

M. M. Ghorab; F. A. Ragab; H. I. Heiba; M. G. El-Gazzar; M. G. El-Gazzar

doi:10.1055/s-0031-1295496

Arzneimittelforschung, Inhaltsverzeichnis

Arzneimittelforschung 2012; 62(01): 46-52
DOI: 10.1055/s-0031-1295496

Original Article

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

M. M. Ghorab

¹Department of Drug Radiation Research, National Center for Radiation Research and Technology (NCRRT), Atomic Energy Authority, Cairo, Egypt

³Medicinal, Aromatic and Poisonous Plants Research Center (MAPPRC), College of Pharmacy, King Saud University, Riyadh, Saudi Arabia

,

F. A. Ragab

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

,

H. I. Heiba

¹Department of Drug Radiation Research, National Center for Radiation Research and Technology (NCRRT), Atomic Energy Authority, Cairo, Egypt

,

M. G. El-Gazzar

¹Department of Drug Radiation Research, National Center for Radiation Research and Technology (NCRRT), Atomic Energy Authority, Cairo, Egypt

,

M. G. El-Gazzar

¹Department of Drug Radiation Research, National Center for Radiation Research and Technology (NCRRT), Atomic Energy Authority, Cairo, Egypt

› Institutsangaben

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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Referenzen

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