title: Synthesis, anticancer and radiosensitizing evaluation of some novel sulfonamide derivatives.
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.
authors.affiliation: 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.
authors.forename: Mostafa M
authors.initials: MM
authors.lastname: Ghorab
authors.affiliation: Department of Pharmaceutical and Medicinal Chemistry, Faculty of Pharmacy, Cairo University, Egypt.
authors.forename: Fatma A
authors.initials: FA
authors.lastname: Ragab
authors.affiliation: Department of Drug Radiation Research, National Center for Radiation Research and Technology, Nasr City, Cairo, Egypt.
authors.forename: Helmy I
authors.initials: HI
authors.lastname: Heiba
authors.affiliation: Department of Drug Radiation Research, National Center for Radiation Research and Technology, Nasr City, Cairo, Egypt.
authors.forename: Marwa G
authors.initials: MG
authors.lastname: El-Gazzar
authors.affiliation: Department of Drug Radiation Research, National Center for Radiation Research and Technology, Nasr City, Cairo, Egypt.
authors.forename: Sally S
authors.initials: SS
authors.lastname: Zahran
mesh_terms: D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D049109:Cell Proliferation / Q000187:drug effects; D004305:Dose-Response Relationship, Drug; D004354:Drug Screening Assays, Antitumor; D056945:Hep G2 Cells; D006801:Humans; D015394:Molecular Structure; D011838:Radiation-Sensitizing Agents / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D013329:Structure-Activity Relationship; D013449:Sulfonamides / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*
chemical_list: D000970:Antineoplastic Agents; D011838:Radiation-Sensitizing Agents; D013449:Sulfonamides
keywords: Anticancer; Radiosensitizers; Sulfonamide