Ontology highlight
ABSTRACT:
SUBMITTER: Fang K
PROVIDER: S-EPMC5900342 | biostudies-literature | 2018 Apr
REPOSITORIES: biostudies-literature
Fang Kun K Dong Guoqiang G Li Yu Y He Shipeng S Wu Ying Y Wu Shanchao S Wang Wei W Sheng Chunquan C
ACS medicinal chemistry letters 20180326 4
In order to take advantage of both immunotherapeutic and epigenetic antitumor agents, the first generation of dual indoleamine 2,3-dioxygenase 1 (IDO1) and histone deacetylase (HDAC) inhibitors were designed. The highly active dual inhibitor <b>10</b> showed excellent and balanced activity against both IDO1 (IC<sub>50</sub> = 69.0 nM) and HDAC1 (IC<sub>50</sub> = 66.5 nM), whose dual targeting mechanisms were validated in cancer cells. Compound <b>10</b> had good pharmacokinetic profiles as an o ...[more]