Azumamides A (1) and E (5) belong to the rare class of histone deacetylase (HDAC) inhibitors, typified by a cyclic tetrapeptide core. HDAC inhibitors are unique lead compounds for the development of specific, noncytotoxic antitumor antibiotics. We have developed a successful protocol for the solution-phase synthesis of azumamides A (1) and E (5), establishing unequivocally the configurations of the azumamides, and presented a three-dimensional NMR solution state structure of azumamide E (5).
Total Synthesis of Azumamides A and E
IZZO, Irene;BIFULCO, Giuseppe;DE RICCARDIS, Francesco
2006
Abstract
Azumamides A (1) and E (5) belong to the rare class of histone deacetylase (HDAC) inhibitors, typified by a cyclic tetrapeptide core. HDAC inhibitors are unique lead compounds for the development of specific, noncytotoxic antitumor antibiotics. We have developed a successful protocol for the solution-phase synthesis of azumamides A (1) and E (5), establishing unequivocally the configurations of the azumamides, and presented a three-dimensional NMR solution state structure of azumamide E (5).File in questo prodotto:
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