4-Methylumbelliferone And Its Derived Compounds: A Brief Review Of Their Cytotoxicity

Document Type : Review Articles


Pharmaceutical Chemistry Department, College of Pharmacy, Mosul University, Mosul-41001, Iraq.


Many efforts have been directed toward the isolation of natural products, and using them to synthesize new chemical agents, and explore their cytotoxic attributes. However, finding new chemotherapeutic agents with towering potentials in the terms of high activity and target-selectivity, as well as minimal side effects is still out of hand. To satisfy that, medicinal chemists directed much of their research toward screening the cytotoxic activity of the isolated products and synthetic compounds. One of the most investigated bands of compounds is those belong to coumarin-family. Although most of these family members exhibited characteristic cytotoxic attributes, the compound termed 4-methylumbelliferone and chemically named 7-hydroxy-4-methylcoumarin showed, with its derived compounds, an exceptional activity in cancer therapy. This effect included the ability of these compounds to counteract the mechanisms of the multidrug-tumor resistance, cover the side potentials of the currently used chemotherapeutic drugs, and boost the tumor sensitivity to phototherapy. In this report, we browsed the literature to report the recent advances for the application of 4-methylumbelliferone and its derived compounds as cytotoxic agents and identify the structural requirements for the maximum selectivity versus each cancer-phenotype. The outcomes of this report may help in the direction of research toward designing and synthesizing new 4-methylumbelliferone-derived products exhibiting the best selectivity and green-side potentials.


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