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Potential pharmaceutical drugs in the field of cancer

December 23, 2005

Raquel Villar Becares, in her PhD thesis at the Public University of Navarre, has developed new derivatives of benzo[b]tiophene 1,1-dioxide that enable their application in the pharmaceutical field. Moreover, the researcher tested for the antitumoural activity of these derivatives, concluding that 23 of the 24 compounds analysed proved to be active or very active against one or more of the tumoural cell lines tested.

Treatment of diabetes or high blood pressure

Although benzo[b]tiophene 1,1-dioxide, found in both crude and processed petroleum oil, was first described in 1893, it was not until the 1950s when it was discovered that the benzo[b]tiophene ring and its derivatives had interesting biological activities for possible use as pesticides, plant growth regulators, analgesics and local anaesthetics and antihistamines, amongst others applications.

In the field of medicine, a bright future is predicted for the possible application of these benzotiophene derivatives as antineoplasic agents. In order to enhance their properties as potential pharmaceutical drugs and to make progress in establishing their mode of action, thus, it was necessary to extend the number of known benzo[b]tiophene derivatives. All this with the end aim of exploring possibilities for their application in the pharmaceutical field as anti-cancer drugs.

The PhD proposed a rational design based on various theoretical methods, thrown up by the new derivatives, the activity of which was subsequently tested. In a parallel manner and, as knowledge was gained about their possible mechanism, Raquel Villar proposed the investigation of possible targets using theoretical docking methods on the protein active structure sites. Subsequently, they were evaluated as cytotoxic agents, tNOX inhibitors and carbonic anhydrase inhibitors.

Anti-tumoural activity

The activity of these new derivatives was tested, concluding that 23 of the 24 compounds analysed proved to be active or very active against one or more tumoural cell lines tested. Thus, the in vitro cytotoxic activity of 24 new derivatives of benzo[b]tiophene 1,1-dioxide were determined for activity against, amongst others: human lung and leukemia fibroblasts.

More specifically, a number of compounds had an in vitro cytotoxicity comparable to the commercial antineoplasic, Doxorrubicina, used as a positive control of activity in the trials carried out for tumoural growth inhibition.

Elhuyar Fundazioa