Discovery of IDO1 and DNA dual targeting antitumor agents

Kun Fang, Shanchao Wu, Guoqiang Dong, Ying Wu, Shuqiang Chen, Jianhe Liu, Wei Wang, Chunquan Sheng

Research output: Contribution to journalArticlepeer-review

9 Scopus citations


The development of small molecules for cancer immunotherapy is highly challenging and indoleamine 2,3-dioxygenase 1 (IDO1) represents a promising target. Inspired by the synergistic effects between IDO1 inhibitors and traditional antitumor chemotherapeutics, the first orally active dual IDO1 and DNA targeting agents were designed by the pharmacophore fusion strategy. The bifunctional hybrids exhibited enhanced IDO1 enzyme inhibitory activity and in vitro cytotoxicity as compared to IDO1 inhibitor 1-methyl-tryptophan and DNA alkylating agent melphalan. In a murine LLC tumor model, the dual targeting agents demonstrated excellent antitumor efficacy, highlighting the advantages of this novel design strategy to improve the efficacy of small molecule cancer immunotherapy.

Original languageEnglish (US)
Pages (from-to)9992-9995
Number of pages4
JournalOrganic and Biomolecular Chemistry
Issue number47
StatePublished - 2017
Externally publishedYes

ASJC Scopus subject areas

  • Biochemistry
  • Physical and Theoretical Chemistry
  • Organic Chemistry


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