2. Academic Validation
  3. Discovery of Imidazoisoindole Derivatives as Highly Potent and Orally Active Indoleamine-2,3-dioxygenase Inhibitors

Discovery of Imidazoisoindole Derivatives as Highly Potent and Orally Active Indoleamine-2,3-dioxygenase Inhibitors

  • ACS Med Chem Lett. 2019 Jun 3;10(6):949-953. doi: 10.1021/acsmedchemlett.9b00114.
Wangyang Tu 1,  Fanglong Yang 1,  Guoji Xu 1,  Jiangtao Chi 1,  Zhiwei Liu 1,  Wei Peng 1,  Bing Hu 1,  Lei Zhang 1,  Hong Wan 1,  Nan Yu 1,  Fangfang Jin 1,  Qiyue Hu 1,  Lianshan Zhang 2,  Feng He 1 3,  Weikang Tao 1 3
Affiliations

Affiliations

  • 1 Shanghai Hengrui Pharmaceutical Co., Ltd., 279 Wenjing Road, Shanghai 200245, China.
  • 2 Jiangsu Hengrui Medicine Co., Ltd., Lianyungang, Jiangsu 222047, China.
  • 3 Chengdu Suncadia Medicine Co., Ltd., 88 South Keyuan Road, Chengdu, Sichuan 610000, China.
PMID: 31223453 DOI: 10.1021/acsmedchemlett.9b00114
Abstract

A novel series of imidazoisoindoles were identified as potent indoleamine-2,3-dioxygenase (IDO) inhibitors. Lead optimization toward improving potency and eliminating CYP inhibition resulted in the discovery of lead compound 25, a highly potent IDO Inhibitor with favorable pharmacokinetic properties. In the MC38 xenograft model in hPD-1 transgenic mice, 25 in combination with the anti-PD-1 monoclonal antibody (SHR-1210) achieved a synergistic antitumor effect superior to each single agent.

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