Ontology highlight
ABSTRACT:
SUBMITTER: Chen W
PROVIDER: S-EPMC5767891 | biostudies-literature | 2018 Jan
REPOSITORIES: biostudies-literature
Chen Wei W Dong Guoqiang G Wu Ying Y Zhang Wannian W Miao Chaoyu C Sheng Chunquan C
ACS medicinal chemistry letters 20171214 1
Novel dual nicotinamide phosphoribosyltransferase (NAMPT) and histone deacetylase (HDAC) inhibitors were designed by a pharmacophore fusion approach. The thiazolocarboxamide inhibitors were highly active for both targets. In particular, compound <b>7f</b> (NAMPT IC<sub>50</sub> = 15 nM, HDAC1 IC<sub>50</sub> = 2 nM) showed potent <i>in vivo</i> antitumor efficacy in the HCT116 xenograft model. The study offers a new strategy for multitarget antitumor drug discovery by simultaneously acting on ca ...[more]