23714-62-7Relevant academic research and scientific papers
Discovery of Hydroxyamidine Derivatives as Highly Potent, Selective Indoleamine-2,3-dioxygenase 1 Inhibitors
Jin, Fangfang,Hu, Qiyue,Fei, Hongbo,Lv, Hejun,Wang, Shenglan,Gui, Bin,Zhang, Junzhen,Tu, Wangyang,Zhang, Yun,Zhang, Lei,Wan, Hong,Zhang, Limin,Hu, Bin,Yang, Fanglong,Bai, Chang,He, Feng,Zhang, Lianshan,Tao, Weikang
supporting information, p. 195 - 201 (2021/02/06)
In this study, a series of novel hydroxyamidine derivatives were identified as potent and selective IDO1 inhibitors by structure-based drug design. Among them, compounds 13-15 and 18 exhibited favorable enzymatic and cellular activities. Compound 18 showed improved bioavailability in mouse, rat, and dog (F% = 44%, 58.8%, 102.1%, respectively). With reasonable in vivo pharmacokinetic properties, compound 18 was further evaluated in a transgenic MC38 xenograft mouse model. The combination of compound 18 with PD-1 monoclonal antibody showed a synergistic antitumor effect. These data indicated that compound 18 as a potential cancer immunotherapy agent should warrant further investigation.
A carbonyl wo containing heptafluoro isopropyl ether compound, preparation method and application thereof
-
Paragraph 0102; 0103; 0104; 0115; 0116; 0117, (2017/08/02)
The present invention discloses a heptafluoroisopropyl-containing carbonyl oxime ether compound, which has the following structural general formula (I), wherein each substituent is defined in the instruction. The present invention further provides a preparation method and applications of the compound. The compound of the present invention is particularly suitable for prevention and control of Mythimna separate, AphiscraccivoraKoch, Tetranychus cinnabarinus, cucumber downy mildew bacteria and rice sheath blight disease bacteria.
