145389-08-8Relevant academic research and scientific papers
Substituted benzothieno [2,3-c] tetrahydropyridine derivative and preparation method and application thereof
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Paragraph 0055; 0068, (2018/07/30)
The invention belongs to the technical field of medicinal chemistry and medicines, and relates to a substituted benzothieno [2,3-c] tetrahydropyridine derivative as shown in formula (I), a preparationmethod of the substituted benzothieno [2,3-c] tetrahydr
Discovery of novel 1,2,3,4-tetrahydrobenzo[4, 5]thieno[2, 3-c]pyridine derivatives as potent and selective CYP17 inhibitors
Wang, Mingliang,Fang, Yanjia,Gu, Shoulai,Chen, Fangfang,Zhu, Zhengjiang,Sun, Xun,Zhu, Jidong
, p. 157 - 172 (2017/03/31)
The inhibition of CYP17 to block androgen biosynthesis is a well validated strategy for the treatment of prostate cancer. Herein we reported the design, synthesis and structure–activity relationship (SAR) study for a series of novel 1,2,3,4- tetrahydroben
OPIOID RECEPTOR MODULATORS
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Page/Page column 97; 102; 103, (2016/06/14)
The present invention provides a compound having the structure wherein A is a ring structure, with or without substitution; X1 is C or N; X2 is N, 0, or S; Y1 is H, -(alkyi), -(alkenyl), -(alkynyl), -(cycloalkyi), (haloalkyi), -(alkyl)-O-(alkyl) or -(alky
Arylsulfanyl pyrazolones block mutant SOD1-G93A aggregation. Potential application for the treatment of amyotrophic lateral sclerosis
Chen, Tian,Benmohamed, Radhia,Arvanites, Anthony C.,Ranaivo, Hantamalala Ralay,Morimoto, Richard I.,Ferrante, Robert J.,Watterson, D. Martin,Kirsch, Donald R.,Silverman, Richard B.
experimental part, p. 613 - 622 (2011/03/17)
Amyotrophic lateral sclerosis (ALS) is an orphan neurodegenerative disease currently without a cure. Mutations in copper/zinc superoxide dismutase 1 (SOD1) have been implicated in the pathophysiology of this disease. Using a high-throughput screening assa
Synthesis of functionalized diaryl sulfides based on regioselective one-pot cyclizations of 1,3-bis(trimethylsilyloxy)-1,3-butadienes
Rashid, Muhammad A.,Rasool, Nasir,Adeel, Muhammad,Reinke, Helmut,Fischer, Christine,Langer, Peter
, p. 3782 - 3793 (2008/09/20)
Functionalized diaryl sulfides were prepared based on one-pot cyclizations of 1,3-bis(trimethylsilyloxy)-1,3-butadienes.
Synthesis and anti-HBV activities evaluation of new ethyl 8-imidazolylmethyl-7-hydroxyquinoline-3-carboxylate derivatives in vitro
Liu, Yajing,Zhao, Yanfang,Zhai, Xin,Liu, Xiuping,Sun, Lixue,Ren, Yanxia,Gong, Ping
scheme or table, p. 446 - 452 (2009/04/11)
Some new ethyl 8-imidazolylmethyl-7-hydroxyquinoline-3-carboxylate derivatives have been synthesized and evaluated for their anti-hepatitis B virus (HBV) activities and cytotoxicities in HepG2.2.15 cells stable transfection with HBV. Compounds 13a, 11b, 11c, 12c, 13c, 11g, and 12g inhibited the expression of the viral antigens HBsAg or HBeAg in a low concentration, of which 11c (IC50 = 12.6 μM, SI = 12.4), 12c (IC50 = 3.5 μM, SI = 37.9), and 12g (IC50 = 2.6 μM, SI = 61.6) showed more active abilities to inhibit the replication of HBV DNA than the positive control lamivudine (3TC, IC50 = 343.2 μM, SI = 7.0).
Regioselective synthesis of diaryl sulfides by [3+3] cyclizations of 1,3-bis(trimethylsilyloxy)-1,3-dienes
Rashid, Muhammad A.,Reinke, Helmut,Langer, Peter
, p. 2321 - 2323 (2007/10/03)
Functionalized and sterically encumbered diaryl sulfides were prepared based on [3+3] cyclizations of 1,3-bis(trimethylsilyloxy)-1,3-dienes.
Synthesis and in vitro anti-hepatitis B virus activities of some ethyl 5-hydroxy-1H-indole-3-carboxylates
Zhao, Chunshen,Zhao, Yanfang,Chai, Huifang,Gong, Ping
, p. 2552 - 2558 (2007/10/03)
A series of ethyl 5-hydroxy-1H-indole-3-carboxylates 6A-10 T were synthesized and evaluated for their anti-hepatitis B virus (HBV) activities in 2.2.15 cells. The IC50 and selective index of inhibition on replication of HB
Calcium channel blocking and positive inotropic activities of ethyl 5-cyano-1,4-dihydro-6-methyl-2-[(phenylsulfonyl)methyl]-4-aryl-3-pyrid ine-carboxylate and analogues. Synthesis and structure-activity relationships
Sircar,Gregor,Anderson,Haleen,Shih,Weishaar,Steffen,Pugsley,Taylor
, p. 2248 - 2260 (2007/10/02)
The synthesis and pharmacological evaluation of a series of 2-[(arylsulfonyl)methyl]-4-aryl-5-cyano-1,4-dihydropyridine-3-carboxyl ic acid esters and analogues are described. These compounds possess a unique profile namely, calcium channel blocking and positive inotropic activities in vitro. Compound 54 was selected as the best compound in the series and was studied in detail. The synthesis and biological profiles of enantiomers of 54 are also reported. The data indicate that although the calcium channel blocking property of 54 is stereospecific the positive inotropic activity is not. Examples of 3- and 6-cyano and other closely related 1,4-dihydropyridine derivatives are described and evaluated for comparison and were found to be devoid of dual activities mentioned above.
