88422-74-6Relevant academic research and scientific papers
Novel molecular targeting anti-tumor aza-steroid derivative based on lipid toxicity and preparation and application thereof
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Paragraph 0140; 0142; 0154; 0159; 0174, (2021/08/19)
The invention provides a novel molecular targeting anti-tumor aza-steroid derivative based on lipid toxicity and a preparation method and application thereof, and belongs to the field of chemical medicines. The derivative is a compound as shown in a formula I, or a salt thereof, or a stereoisomer thereof. The compound is low in toxicity or basically non-toxic to normal cells, has an obvious inhibition effect to tumor cell lines, particularly has good lipid toxicity selectivity to tumor cells such as liver cancer, lung cancer and the like in vivo, and has an obvious inhibition effect; meanwhile, the compound can effectively activate SREBP1 and PPAR gamma, inhibit lipid transport MTTP, cause lipid aggregation in tumor cells and cause lipid toxicity of the tumor cells. The compound can be used for treating liver cancer, lung cancer and the like in a molecular targeting manner, is low in toxicity or even non-toxic, and has a good application prospect.
Tetrazanbigen Derivatives as Peroxisome Proliferator-Activated Receptor Gamma (PPARγ) Partial Agonists: Design, Synthesis, Structure-Activity Relationship, and Anticancer Activities
Gan, Linling,Gan, Zongjie,Dan, Yanrong,Li, Yaowei,Zhang, Peiming,Chen, Shanwen,Ye, Zaijun,Pan, Tao,Wan, Chunmei,Hu, Xuelian,Yu, Yu
, p. 1018 - 1036 (2021/02/01)
Tetrazanbigen (TNBG) is a novel sterol isoquinoline derivative with poor water solubility and moderate inhibitory effects on human cancer cell lines via lipoapoptosis induction. Herein, we developed a series of novel TNBG analogues with improved water sol
HETEROCYCLIC COMPOUNDS AND USE THEREOF
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Paragraph 0051-0052, (2019/03/30)
Disclosed are compounds of formula (I) below or pharmaceutically acceptable salts thereof: in which each of variables R1-R6, L, m, and n is defined herein. Also disclosed are a method for treating an opioid receptor-associated condit
HETEROCYCLIC COMPOUNDS AND USE THEREOF
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Paragraph 0056, (2019/07/23)
Disclosed are compounds of formula (I) below or pharmaceutically acceptable salts thereof:in which each of variables R 1 -R 6 , L, m, and n is defined herein. Also disclosed are a method for treating an opioid receptor-associated condition with a compound
Pyridinopyrazine compounds and preparation method thereof, and medical application of pyridinopyrazine compounds
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Paragraph 0049; 0052, (2016/10/07)
The invention relates to the field of pharmaceutical chemistry, particularly a series of pyridinopyrazine compounds (I). The pharmacodynamical test proves that the compounds are used for resisting external oxidation and electrophilic stimulation by activa
Synthesis and biological evaluation of 1,2,3,4-tetrahydroisoquinolines derivatives as monoamine oxidase inhibitors for treatment of Alzheimer's and Parkinson's diseases
Guo, Hongmei,Lu, Zhenhao,Chen, Shiqiang,Yu, Yu
, p. 3651 - 3654 (2015/12/26)
A series of 1,2,3,4-tetrahydroisoquinolines derivatives were synthesized and evaluated their inhibition effect on monoamine oxidase (MAO). The results of pharmacological test revealed that all the five compounds had certain monoamine oxidase inhibitory ac
3-aroylmethylene-2,3,6,7-tetrahydro-1 H -pyrazino[2,1- a ]isoquinolin-4(11b H)-ones as potent Nrf2/ARE inducers in human cancer cells and AOM-DSS treated mice
Xi, Mei-Yang,Jia, Jian-Min,Sun, Hao-Peng,Sun, Zhong-Ying,Jiang, Jie-Wei,Wang, Ya-Jing,Zhang, Min-Ye,Zhu, Jun-Feng,Xu, Li-Li,Jiang, Zheng-Yu,Xue, Xin,Ye, Ming,Yang, Xi,Gao, Yuan,Tao, Lei,Guo, Xiao-Ke,Xu, Xiao-Li,Guo, Qing-Long,Zhang, Xiao-Jin,Hu, Rong,You, Qi-Dong
, p. 7925 - 7938 (2013/11/06)
Nrf2-mediated activation of ARE regulates expression of cytoprotective enzymes against oxidative stress, inflammation, and carcinogenesis. We have discovered a novel structure (1) as an ARE inducer via luciferase reporter assay to screen the in-house data
Enantioselective synthesis of (R)-(-)-praziquantel (PZQ)
Roszkowski, Piotr,Maurin, Jan K.,Czarnocki, Zbigniew
, p. 1415 - 1419 (2007/10/03)
Praziquantel 8 (2-cyclohexylcarbonyl-1,2,3,6,7,11b-hexahydro-4H-pyrazino[2,1-a]isoquinoline-4-one), a powerful anti-worm drug, has been synthesized in its enantiopure form via asymmetric transfer hydrogenation according to the Noyori protocol. Initially, the reduction of prochiral imine 4 afforded product 5 in 62% ee, but a single crystallization amplified the enantiomeric purity to 98% ee. The final (R)-(-)-praziquantel 8 was prepared in three subsequent steps in 56% chemical yield.
