179473-53-1Relevant articles and documents
Discovery of the programmed cell death-1/programmed cell death-ligand 1 interaction inhibitors bearing an indoline scaffold
Qin, Mingze,Cao, Qi,Wu, Xia,Liu, Chunyang,Zheng, Shuaishuai,Xie, Hongbo,Tian, Ye,Xie, Jun,Zhao, Yanfang,Hou, Yunlei,Zhang, Xian,Xu, Boxuan,Zhang, Haotian,Wang, Xiaobo
, (2020)
Inhibiting the programmed cell death-1 (PD-1)/programmed cell death-ligand 1 (PD-L1) pathway is an attractive strategy for tumor immunotherapy. Here, a novel series of indoline-containing compounds were developed, among which, A13 was identified as the most promising PD-1/PD-L1 pathway inhibitor. At the biochemical level, A13 demonstrated strong inhibition of the PD-1/PD-L1 interaction, with an IC50 of 132.8 nM. Notably, it exhibited outstanding immunoregulatory activity, and significantly elevated interferon-γ secretion in a Hep3B/OS-8/hPD-L1 and CD3 T cell co-culture model, without significant toxic effect. Therefore, A13 could be employed as a suitable lead compound for further design of non-peptide inhibitors targeting the PD-1/PD-L1 interaction. In addition, the preliminary structure-activity relationships of these new indoline compounds were investigated in this study, providing valuable information for future drug development.
Indoline compounds and preparing method and application thereof
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, (2019/06/12)
The invention belongs to the technical field of medicines, and discloses indoline compounds having a general formula I in which substitutes R1, R2, R3, R4 and R5 are defined in the specification and apreparing method and application thereof. The indoline
Ring-fused compound, preparation method thereof and application of compound
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Paragraph 0191; 0192; 0193; 0194; 0195, (2019/05/02)
The invention relates to a ring-fused compound or pharmaceutically acceptable salt thereof, ester, a steric isomer, a tautomer, a polymorphic substance, a solvate, a hydrate, a metabolite or prodrug or mixture of the materials, a medicine composition and medicine box product comprising the compound, a preparation method of the compound and an application of the compound to preparation of medicinesfor preventing or treating PD-1/PD-L1 related diseases.