Design and Synthesis of New Non-Steroidal Anti-Inflammatory Drugs with Anti-Cancer Activity on Colon Rectal Cancer Cell Lines HCT-116 and Caco-2
Date of Award
Doctor of Philosophy
Dr. Michael Barcelona
Dr. Sherine Obare
Dr. Margaret Joyce
Dr. Ekkehard Sinn
Equity, social determinants, intemational development evaluation
Colon rectal cancer is one of the most common types of cancer and is the third leading cause of cancer related deaths among western countries. Current chemotherapy treatments are highly toxic and mostly result in only a low percentage of tumor reduction; therefore an effective treatment with low toxicity is needed.
In this study, different innovative new COX-2 inhibitors were synthesized using the frame of biologically active chalcones to which active COX-2 pharmacophores SO2CH3, SO2NH2, SO2NHCOCH3 were added. Additionally, the effect of different alkyl chain lengths and the effect of different electron donors on the binding of the active sites of these compounds with the COX-2 enzyme were measured.
In total, 25 different compounds were synthesized. It was found that the drugs were non-selective towards the COX-2 or COX-1 enzyme. The lack of selectivity towards inhibition didn't affect the effectiveness of the compounds to inhibit the growth of cancer cells indicating that there is more than just the inhibition of the COX-2 involved in the process of inhibiting colon cancer tumors.
Rodríguez Rivera, Wanda Ivette, "Design and Synthesis of New Non-Steroidal Anti-Inflammatory Drugs with Anti-Cancer Activity on Colon Rectal Cancer Cell Lines HCT-116 and Caco-2" (2015). Dissertations. 1194.