The novel compounds represent an excellent starting point for the further optimization and the design of therapeutically effective anti-cancerous drugs.

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A new series of hydroxycoumarin derivatives has been synthesized using conventional synthesis. The syntheses were accelerated by microwave assistance. Yields in both cases were comparable (59–69 %). The structures were established by 1H and 13C NMR spectroscopy and high-resolution mass spectrometry. Five compounds (5-hydroxy-4,7-dimethylcoumarin, 6-acetyl-5-hydroxy-4,7-dimethylcoumarin, 4-(cyanomethoxy)chromen-2-one, 5-(cyanomethoxy)-4,7-dimethylchromen-2-one, and 6-acetyl-5-(cyanomethoxy)-4,7-dimethylchromen-2-one) were assayed for anti-cancer activity. For all presented coumarin derivatives, lipophilicity was measured using reversed-phase TLC in different eluent systems with standardization. In addition, the crystal structure of 6-acetyl-5-hydroxy-4,7-dimethylcoumarin has been solved by X-ray structure analysis of single crystals.Graphical abstract

Cancer is a major public health problem in many countries of the world. It is currently the second leading cause of death in the United States and is expected to surpass heart diseases as the leading cause of death in the next few years (1). Therefore there is a continuous need for the development of new compounds with potential anticancer activity. Carcinogenesis is a complicated process, usually developing over years. The process may be caused by external factors (responsible for up to 80% of cases), and certain genetic factors. In some types of cancer, the overexpression of specific kinases is one of the basic factors of neoplastic transformation. One example is chronic myeloid leukemia (CML), which is a result of genetic mutation leading to formation of pathological BCR-ABL gene encoding a p210 protein, which shows abnormal, increased tyrosine kinase activity. It is assumed that expression of BCR-ABL is an essential factor for neoplastic transformation in CML. The milestone in the treatment of this type of cancer was introduction of selective kinase inhibitors. In the case of CML, tyrosine kinase inhibitor ñ Imatinib (Glivec) due to the high efficacy and good tolerability, it became the ìgold standardî treatment of patients with CML (2).