4937-87-5Relevant articles and documents
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.
Synthesis and characterization of s-triazine cored tripodal keto-oxime and its trinuclear complexes
Uysal, Saban
experimental part, p. 84 - 92 (2011/11/05)
2,4,6-Tris(4-hydroxybenzimino)-1,3,5-triazine (II) has been synthesized by the reaction of 1equiv. melamine (I) and 3equiv. 4-hydroxybenzaldehyde and characterized by means of elemental analysis, 1H NMR, Fourier transform-infrared spectroscopy, and liquid
CASPASE INHIBITORS CONTAINING DICARBONYLAMINO-ISOXAZOLINE
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Page/Page column 17, (2010/10/20)
The present invention relates to a dicarbonylamino-isoxazoline derivative as an inhibitor against various caspases and a therapeutic composition for preventing inflammation and apoptosis comprising the same.