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Hou, Xiyan,Majik, MaheshS.,Kim, Kyunglim,Pyee, Yuna,Lee, Yoonji,Alexander, Varughese,Chung, Hwa-Jin,Lee, Hyuk Woo,Chandra, Girish,Lee, Jin Hee,Park, Seul-gi,Choi, Won Jun,Kim, Hea Ok,Phan, Khai,Gao, Z American ChemicalSociety 2012 Journal of medicinal chemistry Vol.55 No.1
<P>Truncated <I>N</I><SUP>6</SUP>-substituted-4′-oxo-and 4′-thioadenosine derivatives with C2 or C8 substitutionwere studied as dual acting A<SUB>2A</SUB> and A<SUB>3</SUB> adenosinereceptor (AR) ligands. The lithiation-mediated stannyl transfer andpalladium-catalyzed cross-coupling reactions were utilized for functionalizationof the C2 position of 6-chloropurine nucleosides. An unsubstituted6-amino group and a hydrophobic C2 substituent were required for highaffinity at the hA<SUB>2A</SUB>AR, but hydrophobic C8 substitutionabolished binding at the hA<SUB>2A</SUB>AR. However, most of synthesizedcompounds displayed medium to high binding affinity at the hA<SUB>3</SUB>AR, regardless of C2 or C8 substitution, and low efficacyin a functional cAMP assay. Several compounds tended to be full hA<SUB>2A</SUB>AR agonists. C2 substitution probed geometrically throughhA<SUB>2A</SUB>AR docking was important for binding in order of hexynyl> hexenyl > hexanyl. Compound <B>4g</B> was the most potentligand acting dually as hA<SUB>2A</SUB>AR agonist and hA<SUB>3</SUB>AR antagonist, which might be useful for treatment of asthma or otherinflammatory diseases.</P><P><B>Graphic Abstract</B> <IMG SRC='http://pubs.acs.org/appl/literatum/publisher/achs/journals/content/jmcmar/2012/jmcmar.2012.55.issue-1/jm201229j/production/images/medium/jm-2011-01229j_0013.gif'></P><P><A href='http://pubs.acs.org/doi/suppl/10.1021/jm201229j'>ACS Electronic Supporting Info</A></P>
Hou, Xiyan,Lee, Hyuk-Woo,Tosh, Dilip K.,Zhao, Long Xuan,Jeong, Lak-Shin 대한약학회 2007 Archives of Pharmacal Research Vol.30 No.10
Improved syntheses of potent and selective $A_3$ adenosine receptor agonists, CI-IB-MECA and thio-CI-IB-MECA were accomplished from cheap stating material, D-ribose. New synthetic methods were found to be superior to old methods from the viewpoint of use of cheap starting material, number of steps, and overall yields.
Xiyan Hou,Hyuk Woo Lee,Dilip K. Tosh,Long Xuan Zhao,Lak Shin Jeong 대한약학회 2007 Archives of Pharmacal Research Vol.30 No.10
Improved syntheses of potent and selective A3 adenosine receptor agonists, Cl-IB-MECA and thio-Cl-IB-MECA were accomplished from cheap stating material, D-ribose. New synthetic methods were found to be superior to old methods from the viewpoint of use of cheap starting material, number of steps, and overall yields.
Choi, Mun Ju,Chandra, Girish,Lee, Hyuk Woo,Hou, Xiyan,Choi, Won Jun,Phan, Khai,Jacobson, Kenneth A.,Jeong, Lak Shin Royal Society of Chemistry 2011 Organic & biomolecular chemistry Vol.9 No.20
<P>The stereoselective synthesis of truncated 3′-aminocarbanucleosides 4a–d<I>via</I> a stereo- and regioselective conversion of a diol 9 to bromoacetate 11a and their binding affinity towards the human A<SUB>3</SUB> adenosine receptor are described.</P> <P>Graphic Abstract</P><P>The stereoselective synthesis of truncated 3′-aminocarbanucleosides <I>via</I> a stereo- and regioselective conversion of a diol to bromoacetate and their binding affinity towards the human A<SUB>3</SUB> adenosine receptor are described. <IMG SRC='http://pubs.rsc.org/services/images/RSCpubs.ePlatform.Service.FreeContent.ImageService.svc/ImageService/image/GA?id=c1ob05853c'> </P>
Nayak, Akshata,Chandra, Girish,Hwang, Inah,Kim, Kyunglim,Hou, Xiyan,Kim, Hea Ok,Sahu, Pramod K.,Roy, Kuldeep K.,Yoo, Jakyung,Lee, Yoonji,Cui, Minghua,Choi, Sun,Moss, Steven M.,Phan, Khai,Gao, Zhan-Guo American Chemical Society 2014 Journal of medicinal chemistry Vol.57 No.4
<P/><P>Truncated <I>N</I><SUP>6</SUP>-substituted-(<I>N</I>)-methanocarba-adenosine derivatives with 2-hexynyl substitution were synthesized to examine parallels with corresponding 4′-thioadenosines. Hydrophobic N<SUP>6</SUP> and/or C2 substituents were tolerated in A<SUB>3</SUB>AR binding, but only an unsubstituted 6-amino group with a C2-hexynyl group promoted high hA<SUB>2A</SUB>AR affinity. A small hydrophobic alkyl (<B>4b</B> and <B>4c</B>) or <I>N</I><SUP>6</SUP>-cycloalkyl group (<B>4d</B>) showed excellent binding affinity at the hA<SUB>3</SUB>AR and was better than an unsubstituted free amino group (<B>4a</B>). A<SUB>3</SUB>AR affinities of 3-halobenzylamine derivatives <B>4f</B>–<B>4i</B> did not differ significantly, with <I>K</I><SUB>i</SUB> values of 7.8–16.0 nM. <I>N</I><SUP>6</SUP>-Methyl derivative <B>4b</B> (<I>K</I><SUB>i</SUB> = 4.9 nM) was a highly selective, low efficacy partial A<SUB>3</SUB>AR agonist. All compounds were screened for renoprotective effects in human TGF-β1-stimulated mProx tubular cells, a kidney fibrosis model. Most compounds strongly inhibited TGF-β1-induced collagen I upregulation, and their A<SUB>3</SUB>AR binding affinities were proportional to antifibrotic effects; <B>4b</B> was most potent (IC<SUB>50</SUB> = 0.83 μM), indicating its potential as a good therapeutic candidate for treating renal fibrosis.</P>
Asymmetric Synthesis of (−)-6′-β-Fluoro-aristeromycin via Stereoselective Electrophilic Fluorination
Kim, Gyudong,Yoon, Ji-seong,Jarhad, Dnyandev B.,Shin, Young Sup,Majik, Mahesh S.,Mulamoottil, Varughese A.,Hou, Xiyan,Qu, Shuhao,Park, Jiyong,Baik, Mu-Hyun,Jeong, Lak Shin THE AMERICAN CHEMICAL SOCIETY 2017 ORGANIC LETTERS Vol.19 No.21
<P>(-)-6 '-beta-Fluoro-aristeromycin (2), a potent inhibitor of S-adenosylhomocysteine (AdoHcy) hydrolase, has been synthesized via stereoselective electrophilic fluorination followed by a purine base build-up approach. Interestingly, purine base condensation using a cyclic sulfate resulted in a synthesis of (+)-5 '-beta-fluoro-isoaristeromycin (2a). Computational analysis indicates that the fluorine atom controlled the regioselectivity of the purine base substitution.</P>
Jeong, Lak Shin,Shantanu Pal,Choe, Seung Ah,Choi, Won Jun,Kenneth A. Jacobson,Zhan-Guo Gao,Athena M. Klutz,Xiyan Hou,Kim, Hea Ok,Lee, Hyuk Woo,Lee, Sang Kook,Dilip K. Tosh,Moon, Hyung Ryong 이화여자대학교 약학연구소 2009 藥學硏究論文集 Vol.- No.19
Novel D- and L-4´-thioadenosine derivatives lacking the 4´-hydroxymethyl moiety were synthesized, starting from D-mannose and D-gulonic γ-lactone, respectively, as potent and selective species-independent A₃ adenosine receptor (AR) antagonists. Among the novel 4´-truncated 2-H nucleosides tested, a N^(6)-(3-chlorobenzyl) derivative 7c was the most potent at the human A₃ AR (K_(i) = 1.5 nM), but a N^(6)-(3-bromobenzyl) derivative 7d showed the optimal species-independent binding affinity.