A novel series of sulfonamide derivatives bearing a biologically active pyridone, thio- phene, and hydrazone moieties was synthesized and screened for their cytotoxic activity against HepG2 cell line. The most potent compounds in this study 4, 8d, and 8h were evaluated for their radio-sensitizing activity. Keywords Sulfonamide Pyridone Thiophene Hydrazone Anticancer Radiosensitizers Introduction Radiotherapy is the second most successful treatment for cancer next to surgery . Radiation delivers energy to tissues, causing ionization and excitation of atoms. The effect of radiation is exerted through the generation of single and double strand breaks, apoptosis of cells as they progress through the cell cycle and through the generation of short-lived free radicals (ROS), which damage proteins and membranes . It is now well known that in the presence of chemotherapy, an increased response occurs within the irradiated tissue. Pyridones constitute an important class of anticancer agents  as they act through many mechanisms including inhibition of tyrosine kinases such as FGFR and VEGFR, Met and TAM family kinases [4, 5]. They were also identiﬁed as inhibitors of the serine/threonine kinase PIM-1, which plays an important role in cell cycle progression, signal transduction pathways, and apoptosis [6, 7].
Research on Chemical Intermediates – Springer Journals
Published: Feb 15, 2017
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