1701-18-4Relevant articles and documents
Nucleoside analogs useful as PRMT5 inhibitors
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Paragraph 0219; 0221; 0222; 0223; 0224, (2021/08/11)
The invention relates to the technical field of biological medicines, and particularly discloses a nucleoside analogue used as a PRMT5 inhibitor. According to the nucleoside analogue as shown in the formula (I) or the pharmaceutically acceptable salt of the nucleoside analogue, the nucleoside analogue or the pharmaceutically acceptable salt of the nucleoside analogue shows relatively high inhibition on the activity of PRMT5 and can be used for preventing and/or treating PRMT5-mediated diseases, and the PRMT5-mediated diseases comprise cell abnormal proliferative diseases.
2 -trifluoromethyl -4 - amino - quinoline derivative and application thereof
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Paragraph 0032-0036; 0120-0124, (2021/11/10)
The invention discloses 2 -trifluoromethyl -4 - amino - quinoline derivatives and application thereof, and comprises a compound represented by the following general formula I. The prepared compound is used for preparing an anti-tumor active drug, has a go
Design, Synthesis, and Antifungal Evaluation of Novel Quinoline Derivatives Inspired from Natural Quinine Alkaloids
Yang, Guan-Zhou,Zhu, Jia-Kai,Yin, Xiao-Dan,Yan, Yin-Fang,Wang, Yu-Ling,Shang, Xiao-Fei,Liu, Ying-Qian,Zhao, Zhong-Min,Peng, Jing-Wen,Liu, Hua
, p. 11340 - 11353 (2019/10/14)
Inspired by quinine and its analogues, we designed, synthesized, and evaluated two series of quinoline small molecular compounds (a and 2a) and six series of quinoline derivatives (3a-f) for their antifungal activities. The results showed that compounds 3e and 3f series exhibited significant fungicidal activities. Significantly, compounds 3f-4 (EC50 = 0.41 μg/mL) and 3f-28 (EC50 = 0.55 μg/mL) displayed the superior in vitro fungicidal activity and the potent in vivo curative effect against Sclerotinia sclerotiorum. Preliminary mechanism studies showed that compounds 3f-4 and 3f-28 could cause changes in the cell membrane permeability, accumulation of reactive oxygen species, loss of mitochondrial membrane potential, and effective inhibition of germination and formation of S. sclerotiorum sclerotia. These results indicate that compounds 3f-4 and 3f-28 are novel potential fungicidal candidates against S. sclerotiorum derived from natural products.