| Article ID | Journal | Published Year | Pages | File Type |
|---|---|---|---|---|
| 1376539 | Bioorganic & Medicinal Chemistry Letters | 2008 | 7 Pages |
Abstract
A series of novel 9-substituted camptothecins derived from 9-formylcamptothecin were synthesized. The aldehyde was obtained from 10-hydroxycamptothecin or, better, by total synthesis. The compounds showed antiproliferative activity higher than that of the reference compound topotecan. Modelling suggested the possibility of a favourable interaction of small and polar 9-substituents with the topoisomerase I–DNA complex, which is consistent with the higher activity of these derivatives with respect to the corresponding 7-substituted camptothecins.
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Related Topics
Physical Sciences and Engineering
Chemistry
Organic Chemistry
Authors
Sabrina Dallavalle, Daniela Granza Rocchetta, Loana Musso, Lucio Merlini, Gabriella Morini, Sergio Penco, Stella Tinelli, Giovanni Luca Beretta, Franco Zunino,