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Chandra, Girish,Moon, Yang Won,Lee, Yoonji,Jang, Ji Yong,Song, Jayoung,Nayak, Akshata,Oh, Kawon,Mulamoottil, Varughese A.,Sahu, Pramod K.,Kim, Gyudong,Chang, Tong-Shin,Noh, Minsoo,Lee, Sang Kook,Choi, American Chemical Society 2015 Journal of medicinal chemistry Vol.58 No.12
<P>On the basis of the potent inhibitory activity of neplanocin A (1) against S-adenosylhomocysteine (AdoHcy) hydrolase, we analyzed the comprehensive structure-activity relationships by modifying the adenine and carbasugar moiety of 1 to find the pharmacophore in the active site of the enzyme. The introduction of 7-deazaadenine instead of adenine eliminated the inhibitory activity against the AdoHcy hydrolase, while 3-deazaadenine maintained the inhibitory activity of the enzyme, indicating that N-7 is essential for its role as a hydrogen bonding acceptor. The substitution of hydrogen at the 6'-position with fluorine increased the inhibitory activity Of the enzyme. The one-carbon homologation at the 5'-position generally decreased the inhibitory activity of the enzyme, indicating that steric repulsion exists. A molecular docking study also supported these experimental data. In this study, 6'-fluoroneplanocin A (2) was the most potent inhibitor of AdoHcy hydrolase (IC50 = 0.24 mu M). It showed a potent anti-VSV activity (EC50 = 0.43 mu M) and potent anticancer activity in all the human tumor cell lines tested.</P>
Improved Synthesis of a DNA-dependent Protein Kinase Inhibitor IC86621
Girish Chandra,정낙신,Varughese Alexander,Hyuk Woo Lee 대한약학회 2012 Archives of Pharmacal Research Vol.35 No.4
An improved synthesis of DNA-dependent protein kinase inhibitor, IC86621 is described. This developed method provides an easy access to this simple molecule by using amination, acetylation and Fries rearrangement reactions.
Girish Chandra Pant 강원대학교 산림과학연구소 2014 Journal of Forest Science Vol.30 No.3
Collection of lichen together with tree twigs of oak and other trees bearing abundant growth of lichens is a common practice among the villagers and the rivals residing near Oak forests in Kumaun Himalaya. Nainital forest division represents about Twenty nine percent vegetation of the Oak forest in Kumaun Himalaya. In Kumaun, the lichen trade share is decreasing at an alarming rate of 21.93% which requires immediate actions by the Government. Lichen contributed significantly to household earnings with off-farm activities and this sector was found second highest income creator after Agriculture. It is a source of cash income during the season of extraction, which increases economic access to food. It has been observed in the present study that the secondary collector and transporters together get maximum share (>50%) of income generated from lichen, thus economic exploitation of the poorly educated people by the traders was still prevalent in the area. To improve the socio-economic standard of the people of Kumaun, it may is necessary to increase and improve the lichens resources of the area. There is a strong need for scientific management, best harvesting practices and strict monitoring of resources. The present study was conducted to assess the present and future resource potential for the conservation and sustainable management of lichens, existing market mechanism, role of Lichens in economic upliftment and livelihood generation of rural communities in Kumaun Himalaya.
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>
Pant, Girish Chandra Institute of Forest Science 2014 Journal of Forest Science Vol.30 No.3
Collection of lichen together with tree twigs of oak and other trees bearing abundant growth of lichens is a common practice among the villagers and the rivals residing near Oak forests in Kumaun Himalaya. Nainital forest division represents about Twenty nine percent vegetation of the Oak forest in Kumaun Himalaya. In Kumaun, the lichen trade share is decreasing at an alarming rate of 21.93% which requires immediate actions by the Government. Lichen contributed significantly to household earnings with off-farm activities and this sector was found second highest income creator after Agriculture. It is a source of cash income during the season of extraction, which increases economic access to food. It has been observed in the present study that the secondary collector and transporters together get maximum share (>50%) of income generated from lichen, thus economic exploitation of the poorly educated people by the traders was still prevalent in the area. To improve the socio-economic standard of the people of Kumaun, it may is necessary to increase and improve the lichens resources of the area. There is a strong need for scientific management, best harvesting practices and strict monitoring of resources. The present study was conducted to assess the present and future resource potential for the conservation and sustainable management of lichens, existing market mechanism, role of Lichens in economic upliftment and livelihood generation of rural communities in Kumaun Himalaya.
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>
Quantile estimation using near optimal unbalanced ranked set sampling
Nautiyal, Raman,Tiwari, Neeraj,Chandra, Girish The Korean Statistical Society 2021 Communications for statistical applications and me Vol.28 No.6
Few studies are found in literature on estimation of population quantiles using the method of ranked set sampling (RSS). The optimal RSS strategy is to select observations with at most two fixed rank order statistics from different ranked sets. In this paper, a near optimal unbalanced RSS model for estimating p<sup>th</sup>(0 < p < 1) population quantile is proposed. Main advantage of this model is to use each rank order statistics and is distributionfree. The asymptotic relative efficiency (ARE) for balanced RSS, unbalanced optimal and proposed near-optimal methods are computed for different values of p. We also compared these AREs with respect to simple random sampling. The results show that proposed unbalanced RSS performs uniformly better than balanced RSS for all set sizes and is very close to the optimal RSS for large set sizes. For the practical utility, the near optimal unbalanced RSS is recommended for estimating the quantiles.
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>
Naik, Siddhi D.,Chandra, Girish,Sahu, Pramod K.,Kim, Hong-Rae,Qu, Shuhao,Yoon, Ji-seong,Jeong, Lak Shin The Royal Society of Chemistry 2016 ORGANIC CHEMISTRY FRONTIERS Vol.3 No.11
<▼1><P>Synthesis of 3′-<I>C</I>-substituted-(<I>N</I>)-methanocarba adenosines using stereoselective cyclopropanation, stereoselective nucleophilic addition, regioselective isopropylidene cleavage and regioselective cyclic sulfate condensation.</P></▼1><▼2><P>Stereo- and regio-selective synthesis of 3′-<I>C</I>-substituted-(<I>N</I>)-methanocarba adenosines 3a–c as potential anticancer agents was achieved by employing stereoselective cyclopropanation, stereoselective nucleophilic addition, regioselective isopropylidene cleavage and regioselective base condensation of cyclic sulfate as key steps.</P></▼2>
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>