Synthesis, COX-1/2 inhibition and antioxidant activities of new oxicam analogues designed as potential chemopreventive agents

  • Berenika Marta Szczęśniak-Sięga Department of Chemistry of Drugs, Wroclaw Medical University, Borowska 211, 50-556 Wrocław, Poland;
  • Katarzyna Gębczak Department of Basic Medical Sciences, Wroclaw Medical University, Borowska 211, 50-556 Wrocław, Poland;
  • Tomasz Gębarowski Department of Basic Medical Sciences, Wroclaw Medical University, Borowska 211, 50-556 Wrocław, Poland;
  • Jadwiga Maniewska Department of Chemistry of Drugs, Wroclaw Medical University, Borowska 211, 50-556 Wrocław, Poland;
Keywords: synthesis, chemoprevention, antioxidant, COX, NSAIDs, oxicams


Oxicams (e.g. piroxicam, meloxicam) are widely used nonsteroidal anti-inflammatory drugs (NSAIDs). A large body of evidence from epidemiological and preclinical studies has shown that NSAIDs have a chemopreventive effect on different types of  cancer, especially in colorectal cancer. Moreover  mounting evidence from preclinical and clinical studies suggests that persistent inflammation functions as a driving force in the journey to cancer. What is more, inflammation induces reactive oxygen and nitrogen species, which cause damage to important cellular components (e.g., DNA, proteins and lipids), which can directly or indirectly contribute to malignant cell transformation. In this study, we discuss the synthesis and the resultant newly synthesised oxicam derivatives which are potentially chemopreventive, and at the same time antioxidant. Compound 9c with highest therapeutic index in the LoVo cancer cell line was found to be the most efficient at ROS scavenging activity in the condition of oxidative stress.


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