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Simplified dynemicin analogues: diastereoselective synthesis and evaluation of their activity against plasmid DNA
1Dipartimento di Chimica e Chimica Industriale, via Dodecaneso 31, 16146 Genova, Italy. guanti@chimica.unige.it
Abstract:
The total synthesis of two diastereoisomeric simplified dynemicin analogues is reported. The key steps involved are: the regio- and diastereoselective functionalisation of an appropriate racemic quinoline precursor and the ring closure to give the 10-membered enediyne moiety through a Pd(0)-catalysed Stille reaction. After the successful conversion of one of these derivatives into a compound more readily activable under nearly physiological conditions, the activity against plasmid DNA was evaluated.
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