- Tetrazanbigen Derivatives as Peroxisome Proliferator-Activated Receptor Gamma (PPARγ) Partial Agonists: Design, Synthesis, Structure-Activity Relationship, and Anticancer Activities
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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
- Gan, Linling,Gan, Zongjie,Dan, Yanrong,Li, Yaowei,Zhang, Peiming,Chen, Shanwen,Ye, Zaijun,Pan, Tao,Wan, Chunmei,Hu, Xuelian,Yu, Yu
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p. 1018 - 1036
(2021/02/01)
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- Novel molecular targeting anti-tumor aza-steroid derivative based on lipid toxicity and preparation and application thereof
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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.
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Paragraph 0140; 0142; 0143; 0148; 0149; 0173
(2021/08/19)
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- Novel 2,4-diaminopyrimidines bearing fused tricyclic ring moiety for anaplastic lymphoma kinase (ALK) inhibitor
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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
- 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
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supporting information
p. 2185 - 2191
(2017/04/27)
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- Synthesis and structure activity relationship of tetrahydroisoquinoline- based potentiators of GluN2C and GluN2D containing N-Methyl-D-aspartate receptors
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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
- Santangelo Freel, Rose M.,Ogden, Kevin K.,Strong, Katie L.,Khatri, Alpa,Chepiga, Kathryn M.,Jensen, Henrik S.,Traynelis, Stephen F.,Liotta, Dennis C.
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supporting information
p. 5351 - 5381
(2013/07/26)
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- 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
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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
- 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
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p. 7925 - 7938
(2013/11/06)
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- 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
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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.
- Lv, Hong-Shui,Kong, Xiang-Qian,Ming, Qian-Qian,Jin, Xing,Miao, Jun-Ying,Zhao, Bao-Xiang
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scheme or table
p. 844 - 849
(2012/03/26)
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- Novel formation of 1,3-oxazepine heterocycles via palladium-catalyzed intramolecular coupling reaction
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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.
- Ma, Chen,Liu, Shao-Jie,Xin, Liang,Falck,Shin, Dong-Soo
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p. 9002 - 9009
(2007/10/03)
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- Synthesis and biological evaluation of pyridooxazine-tetrahydroisoquinoline derivatives as MDR modulators
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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
- Ma, Chen,Liu, Shao-Jie,Xin, Liang,Zhang, Qun,Ding, Kai,Falck,Shin, Dong-Soo
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p. 1010 - 1011
(2007/10/03)
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- MACROCYCLIC CARBOXYLIC ACIDS AND ACYLSULFONAMIDES AS INHIBITORS OF HCV REPLICATION
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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.
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Page/Page column 191-192
(2008/06/13)
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- Macrocyclic compounds as inhibitors of viral replication
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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.
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- Synthesis of a small library of phenylalkylamide derivatives as melatoninergic ligands for human mt1 and MT2 receptors
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Focused small libraries of melatonin receptor ligands from arylalkylamine derivatives were synthesised by combinatorial chemistry using the mix and split method in the solid phase. A library of 108 compounds was then synthesised from 12 arylalkyl amines and nine carboxylic acids. The compound mixtures were evaluated on chicken brain melatonin and recombinant human mt1 and MT2 receptors. Deconvolution of the most potent mixture demonstrated the superiority of 3-methoxy and 2,5-dimethoxy substitution on the phenyl ring with isopropyl, propyl and ethyl amido chains. Several compounds with nanomolar affinity for human melatonin receptors were obtained. (C) 2000 Elsevier Science Ltd.
- Pegurier, C.Ecile,Curtet, Sophie,Nicolas, Jean-Paul,Boutin, Jean A.,Delagrange, Philippe,Renard, Pierre,Langlois, Michel
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p. 163 - 171
(2007/10/03)
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- Substituted 1-(aminomethyl)-2-(arylacetyl)-1,2,3,4- tetrahydroisoquinolines: A novel class of very potent antinociceptive agents with varying degrees of selectivity for κ and μ opioid receptors
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This study describes the synthesis of a series of novel substituted 1- (aminomethyl)-2-(arylacetyl)-1,2,3,4-tetrahydroisoquinolines, and discusses their structure-activity relationships (SARs) using binding affinity for opioid receptors and antinociceptive potency as the indices of biological activity. The introduction of a hydroxy substituent in position 5 of the isoquinoline nucleus generated a compound, 40, which is 2 times more potent than the previously disclosed unsubstituted analogue 39 in mouse models of antinociception. A QSAR analysis of the 5-substitution clearly demonstrates that antinociceptive activity is inversely associated with the lipophilicity of the substituents. The substituted compounds described herein are less selective for the κ opioid receptors than the unsubstituted isoquinoline 39. For example, the 5-hydroxy-substituted compound 59 shows high affinity for κ opioid receptors (K(i) κ = 0.09 nM) and a (K(i) μ/K(i) κ ratio of only 5. However, a multiple linear regression analysis demonstrates a lack of correlation between antinociceptive activity and affinity for the μ opioid receptor. On the other hand, the correlation between binding affinity to κ opioid receptor and antinociceptive activity was statistically significant.
- Vecchietti,Clarke,Colle,Dondio,Giardina,Petrone,Sbacchi
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p. 2970 - 2978
(2007/10/02)
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