Synthesis and cytotoxic activity of a new series of topoisomerase I inhibitors |
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Authors: | Dallavalle Sabrina Gattinoni Sonia Mazzini Stefania Scaglioni Leonardo Merlini Lucio Tinelli Stella Beretta Giovanni L Zunino Franco |
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Institution: | Dipartimento di Scienze Molecolari Agroalimentari, Università di Milano, via Celoria 2, 20133 Milano, Italy. |
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Abstract: | A series of structurally simple analogues of natural topopyrone C were synthesized and tested for cytotoxic and topoisomerase I inhibitory activities. The removal of the hydroxyl groups at the 5 and 9 positions resulted in an increased cytotoxic potency and ability to stabilize topoisomerase-mediated cleavage. In addition, the results suggest that some structural features, such as the pyrone ring and a polar group in position 11, are fundamental for topoisomerase I inhibitory effect. These structural requirements are also consistent with the cytotoxic activity. |
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