Antibacterial and Anticancer Activity, Acute Toxicity, and Solubility of Co-crystals of 5-Fluorouracil and Trimethoprim

[Image: see text] 5-Fluorouracil is mainly used for the treatment of tumors and has relatively high toxicity. Trimethoprim is a common broad-spectrum antibiotic agent with extremely poor water solubility. We hoped to solve these problems by synthesizing co-crystals (compound 1) of 5-fluorouracil and trimethoprim. Solubility tests showed that the solubility of compound 1 was improved compared to that of trimethoprim. In vitro anticancer activity tests of compound 1 showed higher activity against human breast cancer cells than 5-fluorouracil. Acute toxicity showed that its toxicity was much lower than that of 5-fluorouracil. In the test of anti-Shigella dysenteriae activity, compound 1 showed much stronger antibacterial activity than trimethoprim.