Synthesis and cytotoxic activity of non-naturally substituted 4-oxycoumarin derivatives

S. Serra, G. Delogu, L. Casu, S. Vázquez-Rodríguez, L. Santana, E. Uriarte, A. Chicca, J. Gertsch

Research output: Contribution to journalArticlepeer-review


Coumarins are a large family of natural and synthetic compounds exerting different pharmacological effects, including cytotoxic, anti-inflammatory or antimicrobial. In the present communication we report the synthesis of a series of 12 diversely substituted 4-oxycoumarin derivatives including methoxy substituted 4-hydroxycoumarins, methyl, methoxy or unsubstituted 3-aryl-4-hydroxycoumarins and 4-benzyloxycoumarins and their anti-proliferative effects on breast adenocarcinoma cells (MCF-7), human promyelocytic leukemia cells (HL-60), human histiocytic lymphoma cells (U937) and mouse neuroblastoma cells (Neuro2a). The most potent bioactive molecule was the 4-hydroxy-5,7- dimethoxycoumarin (compound 1) which showed similar potency (IC 0.2-2 μM) in all cancer cell lines tested. This non-natural product reveals a simple bioactive scaffold which may be exploited in further studies.
Original languageEnglish
Pages (from-to)5791-5794
Number of pages4
JournalBioorganic & Medicinal Chemistry Letters
Issue number18
Publication statusPublished - 15 Sep 2012


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