85553-53-3Relevant articles and documents
Design and optimisation of a small-molecule TLR2/4 antagonist for anti-tumour therapy
Chen, Hekai,Kong, Jun,Li, Tian,Xu, Qun,Yin, Hang,Zhang, Liwei
supporting information, p. 1771 - 1779 (2021/11/19)
In anti-tumour therapy, the toll-like receptor 2/4 (TLR2/4) signalling pathway has been a double-edged sword. TLR2/4 agonists are commonly considered adjuvants for immune stimulation, whereas TLR2/4 antagonists demonstrate more feasibility for anti-tumour therapy under specific chronic inflammatory situations. In individuals with cancer retaliatory proliferation and metastasis after surgery, blocking the TLR2/4 signalling pathway may produce favourable prognosis for patients. Therefore, here, we developed a small-molecule co-inhibitor that targets the TLR2/4 signalling pathway. After high-throughput screening of a compound library containing 14 400 small molecules, followed by hit-to-lead structural optimisation, we finally obtained the compound TX-33, which has effective inhibitory properties against the TLR2/4 signalling pathways. This compound was found to significantly inhibit multiple pro-inflammatory cytokines released by RAW264.7 cells. This was followed by TX-33 demonstrating promising efficacy in subsequent anti-tumour experiments. The current results provide a novel understanding of the role of TLR2/4 in cancer and a novel strategy for anti-tumour therapy.
2-(aryl (azacycloalkane-1-yl) methyl) phenol derivatives and uses thereof
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Paragraph 0371-0374; 0375-0377, (2021/07/24)
The invention discloses 2-(aryl (azacycloalkane-1-yl) methyl) phenol derivatives and application thereof, and belongs to the technical field of medicines. The invention provides a compound shown in a formula I or pharmaceutically acceptable salt thereof. The series of compounds have good inhibitory activity on the histone demethylase KDM4 family in vitro, the median inhibitory concentration (IC50) of most molecules on KDM4D is less than 500 nM, and the compounds have good inhibitory effect on proliferation of various human tumor cell strains in vitro, so that the series of compounds provide a new effective choice for developing targeted histone demethylase KDM4D drugs and preparing drugs for treating and/or preventing cancers and reproductive system diseases, and have good application prospects.
Ruthenium-Catalyzed meta-Selective CAr-H Bond Formylation of Arenes
Jia, Chunqi,Wu, Nini,Cai, Xiaofeng,Li, Gang,Zhong, Lei,Zou, Lei,Cui, Xiuling
, p. 4536 - 4542 (2020/04/09)
The meta-CAr-H bond formylation of arenes has been achieved using CHBr3 as a formyl source in the presence of [Ru(p-cym)(OAc)2] as a catalyst. This method provides efficient access to the preparation of various meta-substituted aromatic compounds, such as alcohols, ethers, amines, nitriles, alkenes, halogens, carboxylic acids, and their derivatives, through transformation of the versatile formyl group. Furthermore, mechanistic studies show that the key active species is a pentagonal ruthenacycle complex.
