Synthesis of Novel Ibuprofen-Tranexamic Acid Codrug: Estimation of The Clinical Activity Against HCT116 Colorectal Carcinoma Cell Line and The Determination of Toxicity Profile Against MDCK Normal Kidney Cell Line

Abstract

Objective: Both ibuprofen and tranexamic acid were tried to treat colorectal carcinoma, however, combined drugs were not. Accordingly, with the aid of SciFinder®, online absence of the mutual prodrug (codrug) was affirmed. This persuade the authors to conduct this research. Methods: The ibuprofen-tranexamic acid codrug was synthesized and characterized with 83% yield. The purified white powder codrug was tested against HCT116 colorectal cancerous cell line and MDCK normal non-cancerous cell line. Results: The newly synthesized and characterized ibuprofen-tranexamic acid codrug has significant parameters. One of which it absolutely obeyes the Lipinski rule of five. Moreover, like the Lipinski rule of five, the number of rotatable bonds (7 rotatable bonds) and the topological polar surface area tPSA (66.4 A2) shows a very favourable oral absorption drug candidate. The IC50 of the mutual prodrug against HCT116 colorectal cells was 5.33 mg/ml, while the IC50 for the MDCK normal kidney cell line was 6.4 g/ml. Conclusion: The authors conclude that the newly synthesized ibuprofen-tranexamic acid codrug has fair anticancer activity against HCT116 colorectal cancer cell line with tolerated toxicity profile acquired with the MDCK normal kidney cell line.