Despite recent advances in understanding cancer biology available therapeutic procedures remain insufficient. Chemotherapy is often accompanied by serious side effects negatively affecting the treatment outcome. Moreover, in view of the commonly occurring phenomenon of resistance to cancer chemotherapeutic agents, there is an acute need for new treatment strategies preventing or reversing the drug resistance. The discovery and development of new, efficient and safe antitumor agents is necessary. We investigated the anticancer activity of derivatives of 4-deoxymonosaccharides equipped with exocyclic enone functionality and coupled to thiophene, bromothiophene and pyrrole.. All novel synthesized compounds (named as FCP28, 29 and 30 and presented on Figure 1) were evaluated for their in vitro anticancer activity against variety of cancer cell lines. We used the human breast cancer cell line (MCF7), human epitheloid cervix carcinoma (HeLa), human ovarian carcinoma (A2780) and a variant of ovarian carcinoma resistant to cisplatin (A2780cis). Cancer cells were incubated in the presence of increasing concentrations of tested compounds for 72h. Next, the IC50 value was calculated using the colorimetric cell viability assay CCK-8 and BioDataFit software. The anticancer potential of studied compounds varied - the most promising compound was FCP28. The most sensitive cell line was HeLa (FCP28: IC50=89 μM and FCP29: IC50=102 μM). It was noticed that FCP28 also killed efficiently human ovarian carcinoma resistant cells ( calculated IC50 was 197 μM). These obtained data clearly show that FCP28 and FCP29 have promising anticancer properties. However, the mechanism of their anticancer action still needs to be evaluated.

Anticancer activity of exo-cyclic carbohydrate enones containing thiophene and pyrolle moieties

253rd National Meeting (2017)

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