Total Synthesis of Solandelactones A and B

The total synthesis of solandelactones A and B is presented. The eastern cyclopropyl moiety was prepared following an exceptionally short chemoenzymatic approach whereas enantioselective synthesis of the western side-chain relied on the application of diastereomerically pure allyl boronates. The natural products solandelactones A and B were isolated in good overall yields following convergence of each eastern and western element by application of the Nozaki–Hiyama–Kishi reaction

Multicomponent Synthesis and Binding Mode of Imidazo[1,2‑<i>a</i>]pyridine-Capped Selective HDAC6 Inhibitors

The multicomponent synthesis of a mini-library of histone deacetylase inhibitors with imidazo­[1,2-<i>a</i>]­pyridine-based cap groups is presented. The biological evaluation led to the discovery of the hit compound MAIP-032 as a selective HDAC6 inhibitor with promising anticancer activity. The X-ray structure of catalytic domain 2 from Danio rerio HDAC6 complexed with MAIP-032 revealed a monodentate zinc-binding mode

Multicomponent Synthesis and Binding Mode of Imidazo[1,2‑<i>a</i>]pyridine-Capped Selective HDAC6 Inhibitors

The multicomponent synthesis of a mini-library of histone deacetylase inhibitors with imidazo­[1,2-<i>a</i>]­pyridine-based cap groups is presented. The biological evaluation led to the discovery of the hit compound MAIP-032 as a selective HDAC6 inhibitor with promising anticancer activity. The X-ray structure of catalytic domain 2 from Danio rerio HDAC6 complexed with MAIP-032 revealed a monodentate zinc-binding mode