6cgp

Publication Abstract from PubMed

The multicomponent synthesis of a mini-library of histone deacetylase inhibitors with imidazo[1,2- a]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- a]pyridine-Capped Selective HDAC6 Inhibitors.,Mackwitz MKW, Hamacher A, Osko JD, Held J, Scholer A, Christianson DW, Kassack MU, Hansen FK Org Lett. 2018 Jun 1;20(11):3255-3258. doi: 10.1021/acs.orglett.8b01118. Epub, 2018 May 23. PMID:29790770^[1]

From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.