Anticancer and radio-sensitizing evaluation of some new sulfonamide derivatives bearing pyridone, thiophene, and hydrazone moieties

Anticancer and radio-sensitizing evaluation of some new sulfonamide derivatives bearing pyridone,... 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 [1]. 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 [2]. 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 [3] 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]. http://www.deepdyve.com/assets/images/DeepDyve-Logo-lg.png Research on Chemical Intermediates Springer Journals

Anticancer and radio-sensitizing evaluation of some new sulfonamide derivatives bearing pyridone, thiophene, and hydrazone moieties

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Publisher
Springer Netherlands
Copyright
Copyright © 2017 by Springer Science+Business Media Dordrecht
Subject
Chemistry; Catalysis; Physical Chemistry; Inorganic Chemistry
ISSN
0922-6168
eISSN
1568-5675
D.O.I.
10.1007/s11164-017-2903-x
Publisher site
See Article on Publisher Site

Abstract

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 [1]. 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 [2]. 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 [3] 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].

Journal

Research on Chemical IntermediatesSpringer Journals

Published: Feb 15, 2017

References

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