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5,6-Fused bicycle-containing heteroaromatics as potential selective anticancer agents: design, synthesis and bioactivity


After cardiovascular diseases, cancer is the second cause of mortality in the world. Thus, it is necessary to study this disease and discover new anticancer drugs.

In this light, our main objectives are to develop new compounds with anticancer potential, fit the nature of the substituents onto the starting materials in certain cases in order to reinforce the metabolic stability of final compounds, to evaluate the anticancer potential of synthesized compounds on tubulin polymerization, on human farnesyltransferase and on cancer cell lines and to establish structure-activity relationships for resulting anticancer agents.

The used strategy is the improvement of the biological activity, by drug-design methods, of ‘hits’ with anticancer potencies (IC50 in the 10-8 molar range), resulting from a previous research work realized by the project leader Pharmacomodulations will be realized on the phenothiazine ring, on the connector and on the benzenic/indole ring via modern synthetic organic methods.

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