http://chineseinput.net/에서 pinyin(병음)방식으로 중국어를 변환할 수 있습니다.
변환된 중국어를 복사하여 사용하시면 됩니다.
A Straightforward Synthesis of K-7174, a GATA-Specific Inhibitor
Majik, Mahesh S.,Yu, Jin-Ha,Jeong, Lak-Shin Korean Chemical Society 2012 Bulletin of the Korean Chemical Society Vol.33 No.9
K-7174, a GATA-specific inhibitor, is a putative anti-inflammatory agent that attenuates effects of inflammatory cytokines in certain cell types. An expeditious four-step synthesis of K-7174 is described in this paper. The route employs Wittig olefination and bis-alkylation of homopiperazine as the key reactions. The iodine-catalyzed isomerization of the Z-isomer results in complete conversion to the E-isomer is the highlight of our synthetic endeavors.
A Straightforward Synthesis of K-7174, a GATA-Specific Inhibitor
Mahesh S. Majik,유진하,정낙신 대한화학회 2012 Bulletin of the Korean Chemical Society Vol.33 No.9
K-7174, a GATA-specific inhibitor, is a putative anti-inflammatory agent that attenuates effects of inflammatory cytokines in certain cell types. An expeditious four-step synthesis of K-7174 is described in this paper. The route employs Wittig olefination and bis-alkylation of homopiperazine as the key reactions. The iodinecatalyzed isomerization of the Z-isomer results in complete conversion to the E-isomer is the highlight of our synthetic endeavors.
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>
Stereoselective Synthesis of Fluoro-homoneplanocin A as a Potential Antiviral Agent
Chandra, Girish,Majik, Mahesh S.,Lee, Ji Yee,Jeong, Lak Shin American Chemical Society 2012 ORGANIC LETTERS Vol.14 No.8
<P>Fluoro-homoneplanocin A (<B>4</B>) was synthesized from <SMALL>d</SMALL>-ribose, via the enyne ring-closing metathesis of <B>9</B>, the stereoselective opening of epoxide <B>23a</B> with fluoride, and a simultaneous oxidation–elimination reaction. The key intermediate <B>8</B> is expected to serve as a versatile intermediate for the synthesis of carbanucleosides.</P><P><B>Graphic Abstract</B> <IMG SRC='http://pubs.acs.org/appl/literatum/publisher/achs/journals/content/orlef7/2012/orlef7.2012.14.issue-8/ol300667q/production/images/medium/ol-2012-00667q_0009.gif'></P><P><A href='http://pubs.acs.org/doi/suppl/10.1021/ol300667q'>ACS Electronic Supporting Info</A></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>
Fluorocyclopentenyl-cytosine with Broad Spectrum and Potent Antitumor Activity<sup>†</sup>
Choi, Won Jun,Chung, Hwa-Jin,Chandra, Girish,Alexander, Varughese,Zhao, Long Xuan,Lee, Hyuk Woo,Nayak, Akshata,Majik, Mahesh S.,Kim, Hea Ok,Kim, Jin-Hee,Lee, Young B.,Ahn, Chang H.,Lee, Sang Kook,Jeon American Chemical Society 2012 Journal of medicinal chemistry Vol.55 No.9
<P>On the basis of the potent biological activity of cyclopentenyl-pyrimidines, fluorocyclopentenyl-pyrimidines were designed and synthesized from <SMALL>d</SMALL>-ribose. Among these, the cytosine derivative <B>5a</B> showed highly potent antigrowth effects in a broad range of tumor cell lines and very potent antitumor activity in a nude mouse tumor xenograft model implanted with A549 human lung cancer cells. However, its 2′-deoxycytidine derivative <B>5b</B> did not show any antigrowth effects, indicating that 2′-hydroxyl group is essential for the biological activity.</P><P><B>Graphic Abstract</B> <IMG SRC='http://pubs.acs.org/appl/literatum/publisher/achs/journals/content/jmcmar/2012/jmcmar.2012.55.issue-9/jm3004009/production/images/medium/jm-2012-004009_0007.gif'></P><P><A href='http://pubs.acs.org/doi/suppl/10.1021/jm3004009'>ACS Electronic Supporting Info</A></P>