34162-12-4Relevant academic research and scientific papers
Novel molecular targeting anti-tumor aza-steroid derivative based on lipid toxicity and preparation and application thereof
-
Paragraph 0140; 0142; 0143; 0148; 0149; 0173, (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
Novel 2,4-diaminopyrimidines bearing fused tricyclic ring moiety for anaplastic lymphoma kinase (ALK) inhibitor
Achary, Raghavendra,Mathi, Gangadhar Rao,Lee, Dong Ho,Yun, Chang Soo,Lee, Chong Ock,Kim, Hyoung Rae,Park, Chi Hoon,Kim, Pilho,Hwang, Jong Yeon
supporting information, p. 2185 - 2191 (2017/04/27)
In this study, a series of novel 2,4-diaminopyrimidines bearing fused tricyclic ring moiety was described for ALK inhibitor. The pyrazole, imidazole, 1,2,4-triazole, piperazine and phenanthridine moieties were employed at the 2-position of pyrimidine. Amo
Synthesis and structure activity relationship of tetrahydroisoquinoline- based potentiators of GluN2C and GluN2D containing N-Methyl-D-aspartate receptors
Santangelo Freel, Rose M.,Ogden, Kevin K.,Strong, Katie L.,Khatri, Alpa,Chepiga, Kathryn M.,Jensen, Henrik S.,Traynelis, Stephen F.,Liotta, Dennis C.
supporting information, p. 5351 - 5381 (2013/07/26)
We describe here the synthesis and evaluation of a series of tetrahydroisoquinolines that show subunit-selective potentiation of NMDA receptors containing the GluN2C or GluN2D subunits. Bischler-Napieralski conditions were employed in the key step for the
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
Synthesis of 5-benzyl-2-phenylpyrazolo[1,5-a]pyrazin-4,6(5H,7H)-dione derivatives and discovery of an apoptosis inducer for H322 lung cancer cells
Lv, Hong-Shui,Kong, Xiang-Qian,Ming, Qian-Qian,Jin, Xing,Miao, Jun-Ying,Zhao, Bao-Xiang
scheme or table, p. 844 - 849 (2012/03/26)
A series of substituted 5-benzyl-2-phenylpyrazolo[1,5-a]pyrazin-4,6(5H,7H)- dione derivatives was synthesized by one-step reaction of ethyl 3-phenyl-1H-pyrazole-5-carboxylate derivatives and N-arylalkyl-2- chloroacetamide. Structures of the compounds were determined by IR, 1H NMR and mass spectroscopy. In addition, a representative single-crystal structure was characterized by using X-ray diffraction analysis. The compound 5j could selectively inhibit the growth of H322 lung cancer cells which contain a mutated p53 gene in a dose-dependent manner through inducing apoptosis of cells.
Novel formation of 1,3-oxazepine heterocycles via palladium-catalyzed intramolecular coupling reaction
Ma, Chen,Liu, Shao-Jie,Xin, Liang,Falck,Shin, Dong-Soo
, p. 9002 - 9009 (2007/10/03)
The oxazepine ring systems containing pyridazinone moiety were constructed via palladium-catalyzed intramolecular coupling reaction. The best conditions for this reaction were Pd(OAc)2 as a palladium source, 1,1′-bis(diphenylphosphino)-ferrocene (DPPF) as the ligand, and K2CO3 as base at 80 °C in toluene. The products have potential applications as biological and medicinal relevant compounds.
Synthesis and biological evaluation of pyridooxazine-tetrahydroisoquinoline derivatives as MDR modulators
Ma, Chen,Liu, Shao-Jie,Xin, Liang,Zhang, Qun,Ding, Kai,Falck,Shin, Dong-Soo
, p. 1010 - 1011 (2007/10/03)
Pyridooxazine-tetrahydroisoquinoline derivatives were designed and synthesized for MDR modulating activity. Pyridooxazin-2-one scaffolds were constructed in a one-pot annulation of N-substituted-2-chloroacetamides with 2-bromo-3-hydroxy pyridine via Smile
Macrocyclic compounds as inhibitors of viral replication
-
, (2008/06/13)
The embodiments provide compounds of the general formulas I-XIX, as well as compositions, including pharmaceutical compositions, comprising a subject compound. The embodiments further provide treatment methods, including methods of treating flaviviral infection, including hepatitis C virus infection and methods of treating liver fibrosis, the methods generally involving administering to an individual in need thereof an effective amount of a subject compound or composition.
MACROCYCLIC CARBOXYLIC ACIDS AND ACYLSULFONAMIDES AS INHIBITORS OF HCV REPLICATION
-
Page/Page column 191-192, (2008/06/13)
The present invention provides compounds of the general formulas I-IX, as well as compositions, including pharmaceutical compositions, comprising a subject compound. The present invention further provides treatment methods, including methods of treating a hepatitis C virus infection and methods of treating liver fibrosis, the methods generally involving administering to an individual in need thereof an effective amount of a subject compound or composition.
