Synthesis and biological characterization of the histone deacetylase inhibitor largazole and C7-modified analogues

…, G Franci, R Álvarez, L Altucci, ÁR de Lera

Index: Souto, Jose A.; Vaz, Esther; Lepore, Ilaria; Poeppler, Ann-Christin; Franci, Gianluigi; Alvarez, Rosana; Altucci, Lucia; De Lera, Angel R. Journal of Medicinal Chemistry, 2010 , vol. 53, # 12 p. 4654 - 4667

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Citation Number: 57

Abstract

Largazole 4a and analogues with modifications at the C7 position, as well as 2, 4′- bithiazole 5a, have been synthesized using an acyclic cross-metathesis of the corresponding depsipeptide structures assembled by N− C6 (O) or C15 (O)-N lactam formation. Similar to the parent system 4a, the series of largazole depsipeptides 4b− d, but not 2, 4′-bithiazole 5a, showed a marked inhibition of recombinant HDAC1 and ...