4 research outputs found
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 imidazoÂ[1,2-<i>a</i>]Âpyridine-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 imidazoÂ[1,2-<i>a</i>]Âpyridine-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