Resveratrol and derivatives Potential antitumor agents?
Resveratrol, stilbenes and derivatives with probable inhibitory activity against human topoisomerase I
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It is well known that natural products play an important role in the discovery of new drugs. The discovery and development of new compounds is a consequence of the rapidly increasing number of molecular targets against which they can be tested. This is why DNA-related enzymes are used as targets to test compounds with possible anticancer and antiviral properties. In the present work, a family of stilbenes was synthesized in order to evaluate their possible inhibitory activity against human Topoisomerase I and Taq DNA polymerase. None of them was able to inhibit "in vitro" human Topoisomerase I...
It is well known that natural products play an important role in the discovery of new drugs. The discovery and development of new compounds is a consequence of the rapidly increasing number of molecular targets against which they can be tested. This is why DNA-related enzymes are used as targets to test compounds with possible anticancer and antiviral properties. In the present work, a family of stilbenes was synthesized in order to evaluate their possible inhibitory activity against human Topoisomerase I and Taq DNA polymerase. None of them was able to inhibit "in vitro" human Topoisomerase I, however, this does not rule out that they may act as inhibitors in some metabolic signaling pathway, as is the case of resveratrol. On the other hand, they were tested against Taq DNA polymerase, 19 of them were able to inhibit the catalytic activity of Taq DNA polymerase. It is postulated that the compounds interact directly with the enzyme and not with DNA, because if it were this way, inhibition of both enzymes would be observed by the generation of conformational changes.
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