Synthesis, anticancer and radiosensitizing evaluation of some novel sulfonamide derivatives

Eur J Med Chem. 2015 Mar 6:92:682-92. doi: 10.1016/j.ejmech.2015.01.036.

Mostafa M Ghorab ¹, Fatma A Ragab ², Helmy I Heiba ³, Marwa G El-Gazzar ³, Sally S Zahran ³

Affiliations

1 Department of Drug Radiation Research, National Center for Radiation Research and Technology, Nasr City, Cairo, Egypt; Department of Pharmacognosy, College of Pharmacy, King Saud University, P.O. Box 2457, Riyadh 11451, Saudi Arabia. Electronic address: mmsghorab@yahoo.com.
2 Department of Pharmaceutical and Medicinal Chemistry, Faculty of Pharmacy, Cairo University, Egypt.
3 Department of Drug Radiation Research, National Center for Radiation Research and Technology, Nasr City, Cairo, Egypt.

PMID: 25618015 DOI: 10.1016/j.ejmech.2015.01.036

Abstract

In this study, novel series of sulfonamide derivatives were synthesized starting from 2-cyanoacetyl)hydrazono)ethyl)phenyl)benzenesulfonamide 4a and 2-cyanoacetyl)hydrazono)ethyl)phenyl)-4-methylbenzenesulfonamide 4b. Different biologically active moieties as pyrazol, thiophene, pyridine and pyrimidines were introduced in order to investigate their in-vitro Anticancer activity, in addition to a novel series of sulfonamide Chalcones were synthesized from the reported 4-acetyl-N-(P-tolyl) benzenesulfonamide 3b. The newly synthesized sulfonamide derivatives were characterized by FT-IR, (1)H NMR, (13)C NMR, mass spectroscopy and elemental analyses and were tested for their in-vitro Anticancer activity against human tumor liver cell line (HEPG-2). The most potent compounds in this study were compounds 4a, 4b, 5a, 6a, 6b, 8, 9, 11, 13, 18 and 19 which showed higher activity than doxorubicin with IC50 ranging from 11.0 to 31.8 μM. Additionally, eight compounds among the most potent were evaluated for their ability to enhance the cell killing effect of γ-radiation.

Keywords

Anticancer; Radiosensitizers; Sulfonamide.

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