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Abstract
5-Fluorouracil (5-FU) is a drug that belong to the antimetabolite class of antineoplastic agents, with a broad spectrum of activity against solid tumors, the use of oral 5-FU was abandoned decades ago because of its irregular absorption and rapid degradation. A potential strategy to improve the selective properties of 5-FU is the chemical transformation into reversible derivatives (prodrugs) which are converted to the parent drug by virtue of enzymatic or chemical means. In the present study, three derivatives of 5-fluorouracil have been designed to be synthesized as an azo derivatives of 5-fluorouracil in order to selectively deliver 5-fluorouracil into the cancer cells of the colon. The synthesis of the target compounds were accomplished following multistep reaction procedures. The chemical reactions were followed up and purity of the products was checked by TLC. The structure of the final compounds and their intermediates were characterized and identified by their melting points, infrared spectroscopy and elemental microanalysis. Compounds 2 and 3 were subjected to a stability study in phosphate buffer (pH 1.5 and 7.8) for different time intervals (0 – 240 min) at 37°C.
Highlights
The aim of most cancer chemotherapeutic drugs currently in clinical use is to kill malignant tumor cells by inhibiting some of the mechanisms implied in cellular division
Colorectal cancer (CRC) is a type of cancer that starts in the colon or rectum portion of large intestine in the gastrointestinal (GI) tract [5].Occurrence of CRC may be dependent on various factors, namely diet, life style and other environmental parameters, including environmental and food-borne mutagens [6]
It is estimated that chronic inflammation, likely to be caused by a dysregulated intestinal microbiota, contributes to approximately 20% of all CRC cases [7, 8]. 5-Fluorouracil (5-FU) is still a widely used anticancer drug
Summary
The aim of most cancer chemotherapeutic drugs currently in clinical use is to kill malignant tumor cells by inhibiting some of the mechanisms implied in cellular division. Various inflammatory mediators are highly expressed in inflammatory tissues, and inflammation-triggered anti-apoptosis activity and cell growth cause cancer development [17] Inflammatory bowel disease, such as ulcerative colitis and Crohn‟s disease is a longstanding inflammatory disease of intestine with increased risk for colorectal cancer (CRC). Colon- specific drug delivery through colon-specific prodrug, activation may be accomplished by the utilization of high activity of certain enzymes at the target site, relative to non-target tissues [24] In view of these observations, three new derivatives of 5-fluorouracil have been designed, synthesized and characterized
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