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Thapa Magar, Til Bahadur,Kadayat, Tara Man,Lee, Hwa-Jong,Park, Seojeong,Bist, Ganesh,Shrestha, Aarajana,Kwon, Youngjoo,Lee, Eung-Seok Elsevier 2017 Bioorganic & medicinal chemistry letters Vol.27 No.15
<P><B>Abstract</B></P> <P>A new series of 2-chloropheny-substituted benzofuro[3,2-<I>b</I>]pyridines were designed, synthesized, and evaluated for topoisomerase I and II inhibition and antiproliferative activity. Compounds <B>17</B>–<B>19, 23, 24, 26,</B> and <B>27</B> exhibited excellent topo II inhibitory activity. A systematic structure-activity relationship study revealed the important role of chlorine substitution in the strong topoisomerase inhibitory activity.</P> <P><B>Graphical abstract</B></P> <P>[DISPLAY OMISSION]</P>
Thapa, P.,Kadayat, T.M.,Park, S.,Shin, S.,Thapa Magar, T.B.,Bist, G.,Shrestha, A.,Na, Y.,Kwon, Y.,Lee, E.S. Academic Press ; Academic Press 2016 Bioorganic chemistry Vol.66 No.-
<P>A new series of 2-phenol-4-chlorophenyl-6-aryl pyridines were designed, synthesized, and evaluated for topoisomerase (topo) I and II inhibitory activities as well as cytotoxic activity against four different human cancer cell lines such as HCT15, T47D, DU145, and Hela. Most of the tested compounds exhibited stronger topo II inhibitory activity at 100 mu M as compared to etoposide. All the compounds, except 39, did not show topo I inhibitory activity. Interestingly, compounds that showed better topo II inhibition than etoposide have ortho-or para-chlorophenyl at 4-position of central pyridine, and none of the compounds possess meta-chlorophenyl. SAR study revealed the importance of ortho-or para-chlorophenyl at 4-position of the central pyridine for selective topo II inhibitory activity. Similarly, all compounds possessing meta-or para-hydroxyphenyl moieties showed moderate to significant cytotoxic effects. Particularly, compounds 27-37, and 39 which showed excellent cytotoxicity (IC50 = 0.68-1.25 mu M) against T47D breast cancer cells suggest the importance of meta-or para-hydroxyphenyl moiety at 2-position of the central pyridine for the design of anticancer agents with related scaffolds. (C) 2016 Elsevier Inc. All rights reserved.</P>
Magar, Til Bahadur Thapa,Seo, Seung Hee,Kadayat, Tara Man,Jo, Hyunji,Shrestha, Aarajana,Bist, Ganesh,Katila, Pramila,Kwon, Youngjoo,Lee, Eung-Seok Elsevier 2018 Bioorganic & medicinal chemistry Vol.26 No.8
<P><B>Abstract</B></P> <P>As part of our effort to develop potential topoisomerase IIα (topo IIα) targeting anticancer agents, we systematically designed a new series of hydroxy and chloro-substituted 2,4-diphenyl 5<I>H</I>-chromeno[4,3-<I>b</I>]pyridines. Total eighteen compounds were synthesized and tested for their ability to inhibit the function of topo I and IIα, and proliferation of human breast (T47D), colorectal (HCT15), and cervix (HeLa) cancer cells. Except compound <B>11</B>, all of the tested compounds displayed selective topo IIα inhibitory activity. Compounds <B>8</B>–<B>18</B>, <B>22</B>, <B>24</B>, and <B>25</B> showed excellent topo IIα inhibitory activity than a positive control, etoposide. Most of the compounds appeared to be superior to reference compounds in their antiproliferative activity. Structure-activity relationship (SAR) study has shown that it is better to place the hydroxyphenyl group at the 4-position of the central pyridine for superior topo IIα inhibition and antiproliferative activity. Similarly, the 3′-, or 4′-hydroxyphenyl substitution at the 2- and 4-positon of pyridine ring is important for better activity than 2′-substitution.</P> <P><B>Highlights</B></P> <P> <UL> <LI> A new series of hydroxy and chloro-substituted 2,4-diphenyl 5<I>H</I>-chromeno[4,3-<I>b</I>]pyridines were synthesized. </LI> <LI> Evaluated for topo I and IIα inhibitory activity, and antiproliferative activity. </LI> <LI> Compounds showed selective topo IIα inhibitory activity. </LI> <LI> SAR study indicated the importance of hydroxyphenyl-substitution at 4-position. </LI> </UL> </P> <P><B>Graphical abstract</B></P> <P>[DISPLAY OMISSION]</P>
( Pritam Thapa ),( Kyu Yeon Jun ),( Tara Man Kadayat ),( Chanmi Park ),( Zhi Zheng ),( Til Bahadur Thapa Magar ),( Ganesh Bist ),( Aarajana Shrestha ),( Younghwa Na ),( Youngjoo Kwon ),( Eung Seok Lee 영남대학교 약품개발연구소 2016 영남대학교 약품개발연구소 연구업적집 Vol.26 No.-
To develop novel selective topoisomerase II inhibitors, we designed and synthesized a series of conforma-tionally constrained hydroxylated 4-phenyl-2-aryl chromenopyridines and evaluated their to poi so-merase inhibitory activity and cytotoxicity against three human cancer cell lines (DU145, HCn5, and T47D) and a normal cell line (MCF10A). All of the prepared compounds displayed stronger or similar topoisomerase II inhibitory activity as well as cytotoxicity against three human cancer cell lines com-pared to etoposide. Compounds 10., 109, 11., 11f, 11g, 12., 12f, and 12g especially showed stronger topoisornerase II inhibitory activity as compared to etoposide at both 100 μM and 20 μM. A structure-ac-tivity relationship study revealed that hydroxyphenyl moiety at 4-position of pyridine and ortho-hydrox-yphenyl or thienyl moiety at 2-position of pyridine has an important role in displaying selective topoisomerase II inhibition. The compound 12b with para-hydroxyphenyl and meta-hydroxyphenyl at 4- and 2-position of pyridine. respectively, showed the most significant cytotoxicity against all three can-cer cell lines, whereas less cytotoxicity to a normal cell line as compared to adriamycin.
Rubin Thapa Magar,송재경 한국미생물·생명공학회 2020 Journal of microbiology and biotechnology Vol.30 No.1
Quercetin and its derivatives are important metabolites that belong to the flavonol class of flavonoids. Quercetin and some of the conjugates have been approved by the FDA for human use. They are widely distributed among plants and have various biological activities, such as being anticancer, antiviral, and antioxidant. Hence, the biosynthesis of novel derivatives is an important field of research. Glycosylation and methylation are two important modification strategies that have long been used and have resulted in many novel metabolites that are not present in natural sources. A strategy for modifying quercetin in E. coli by means of glycosylation, for example, involves overexpressing respective glycosyltransferases (GTs) in the host and metabolic engineering for increasing nucleoside diphosphate sugar (NDP-sugar). Still others have used microorganisms other than E. coli, such as Streptomyces sp., for the biotransformation process. The overall study of the structural activity relationship has revealed that modification of some residues in quercetin decreased one activity but increased others. This review summarizes all of the information mentioned above.
( Pritam Thapa ),( Tara Man Kadayat ),( Seojeong Park ),( Somin Shin ),( Til Bahadur Thapa Magar ),( Ganesh Bist ),( Aarajana Shrestha ),( Younghwa Na ),( Youngjoo Kwon ),( Eung Seok Lee ) 영남대학교 약품개발연구소 2016 영남대학교 약품개발연구소 연구업적집 Vol.26 No.-
A new series of 2-phenol-4-chlorophenyl-6-aryl pyridines were designed, synthesized, and evaluated for topoisomerase (topo) I and II inhibitory activities as well as cytotoxic activity against four different human cancer cell lines such as HCT15, T47D, DU145, and Hela. Most of the tested compounds exhibited stronger topo II inhibitory activity at 100 μM as compared to etoposide. All the compounds, except 39, did not show topo I inhibitory activity. Interestingly, compounds that showed better topo II inhibition than etoposide have ortho- or para-chlorophenyl at 4-position of central pyridine, and none of the com-pounds possess meta-chlorophenyl. SAR study revealed the importance of ortha- or para-chlorophenyl at 4-position of the central pyridine for selective tapa II inhibitory activity. Similarly, all compounds possessing mere- or para-hydroxyphenyl moieties shawed moderate to significant cytotoxic effects. Particularly, compounds 27-37, and 39 which showed excellent cytotoxicity (IC<sub>50</sub> = 0.68-1.25 μM) against T47D breast cancer cells suggest the importance of meta- or para-hydroxyphenyl moiety at 2-position of the central pyridine for the design of anticancer agents with related scaffolds.
Sunny Thapa Magar,Hae Jung Suk 한국콘텐츠학회(IJOC) 2020 International Journal of Contents Vol.16 No.2
In the era of noble technology, virtual reality (VR) has been adopted in various fields, with the advantages of VR in education being confirmed through numerous studies. In skill development training education, humans or equipment that interact with the trainee are crucial and currently VR is more preferred. In this study, six projects were selected and reviewed in-depth visualizing the use of VR in training and its potential. Comparison between the learning actions of training in the virtual and real environments were conducted. Training through VR is location-dependent, time-dependent, safe, and reversible. VR application is also determined by the preps and feedback-providing functionality which must be emphasized. All the advantages of VR in skill development training make it an opportunity provider. This article can be used by those developing VR projects for skill development training.
Til Bahadur Thapa Magar,KADAYAT TARAMAN,오혜진,박필훈,이응석 대한화학회 2017 Bulletin of the Korean Chemical Society Vol.38 No.6
Chromanone-containing compounds have been reported to possess several important biological activities. As a part of our continuing effort for discovering potent anti-inflammatory agents, a series of halogen-containing 3-benzylidenechroman-4-ones (1–15) were synthesized, and evaluated for their inhibitory effect on lipopolysaccharide (LPS)-stimulated reactive oxygen species (ROS) production in RAW 264.7 macrophages. Compounds 4 and 10 exhibited significant inhibitory activity (IC50 = 5.09 ± 1.27 and 5.11 ± 0.51 μM, respectively) against LPS-stimulated ROS production in RAW 264.7 macrophages.