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      • Synthesis, bioevaluation and docking study of 5-substitutedphenyl-1,3,4-thiadiazole-based hydroxamic acids as histone deacetylase inhibitors and antitumor agents

        Nam, Nguyen-Hai,Huong, Tran Lan,Dung, Do Thi Mai,Dung, Phan Thi Phuong,Oanh, Dao Thi Kim,Park, Sang Ho,Kim, Kyungrok,Han, Byung Woo,Yun, Jieun,Kang, Jong Soon,Kim, Youngsoo,Han, Sang-Bae Informa UK Ltd. 2014 Journal of enzyme inhibition and medicinal chemist Vol.29 No.5

        <P>Since the first histone deacetylase (HDAC) inhibitor (Zolinza®, widely known as suberoylanilide hydroxamic acid; SAHA) was approved by the Food and Drug Administration for the treatment of T-cell lymphoma in 2006, the search for newer HDAC inhibitors has attracted a great deal of interest of medicinal chemists worldwide. As a continuity of our ongoing research in this area, we designed and synthesized a series of 5-substitutedphenyl-1,3,4-thiadiazole-based hydroxamic acids as analogues of SAHA and evaluated their biological activities. A number of compounds in this series, for example, <I>N<SUP>1</SUP></I>-hydroxy-<I>N</I><SUP>8</SUP>-(5-(2-chlorophenyl)-1,3,4-thiadiazol-2-yl)octandiamide (<B>5b</B>), <I>N<SUP>1</SUP></I>-hydroxy-<I>N</I><SUP>8</SUP>-(5-(3-chlorophenyl-1,3,4-thiadiazol-2-yl)octandiamide (<B>5c</B>) and <I>N<SUP>1</SUP></I>-hydroxy-<I>N</I><SUP>8</SUP>-(5-(4-chlorophenyl)-1,3,4-thiadiazol-2-yl)octandiamide (<B>5d</B>), were found to possess potent anticancer cytotoxicity and HDAC inhibition effects. Compounds <B>5b</B>-<B>d</B> were generally two- to five-fold more potent in terms of cytotoxicity compared to SAHA against five cancer cell lines tested. Docking studies revealed that these hydroxamic acid displayed higher affinities than SAHA toward HDAC8.</P>

      • The insight of <i>in vitro</i> and <i>in silico</i> studies on cholinesterase inhibitors from the roots of <i>Cimicifuga dahurica</i> (Turcz.) Maxim.

        Kim, Jang Hoon,Thao, Nguyen Phuong,Han, Yoo Kyong,Lee, Young Suk,Luyen, Bui Thi Thuy,Oanh, Ha Van,Kim, Young Ho,Yang, Seo Young TaylorFrancis 2018 Journal of enzyme inhibition and medicinal chemist Vol.33 No.1

        <P><B>Abstract</B></P><P>Cholinesterases (ChEs) are enzymes that break down neurotransmitters associated with cognitive function and memory. We isolated cinnamic acids (<B>1</B> and <B>2</B>), indolinones (<B>3</B> and <B>4</B>), and cycloartane triterpenoid derivatives (<B>5</B>–<B>19</B>) from the roots of <I>Cimicifuga dahurica</I> (Turcz.) Maxim. by chromatography. These compounds were evaluated for their inhibitory activity toward ChEs. Compound <B>1</B> was determined to have an IC<SUB>50</SUB> value of 16.7 ± 1.9 μM, and to act as a competitive inhibitor of acetylcholinesterase (AChE). Compounds <B>3</B>, <B>4</B> and <B>14</B> were found to be noncompetitive with IC<SUB>50</SUB> values of 13.8 ± 1.5 and 6.5 ± 2.5 μM, and competitive with an IC<SUB>50</SUB> value of 22.6 ± 0.4 μM, respectively, against butyrylcholinesterase (BuChE). Our molecular simulation suggested each key amino acid, Tyr337 of AChE and Asn228 of BuChE, which were corresponded with potential inhibitors <B>1</B>, and <B>3</B> and <B>4</B>, respectively. Compounds <B>1</B> and <B>4</B> were revealed to be promising compounds for inhibition of AChEs and BuChEs, respectively.</P>

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        The complete mitochondrial genome sequence of the indigenous I pig (Sus scrofa) in Vietnam

        Hieu Duc Nguyen,Tuan Anh Bui,Phuong Thanh Nguyen,Oanh Thi Phuong Kim,Thuy Thi Bich Vo 아세아·태평양축산학회 2017 Animal Bioscience Vol.30 No.7

        Objective: The I pig is a long nurtured longstanding breed in Vietnam, and contains excellent indigenous genetic resources. However, after 1970s, I pig breeds have become a small population because of decreasing farming areas and increasing pressure from foreign breeds with a high growth rate. Thus, there is now the risk of the disappearance of the I pigs breed. The aim of this study was to focus on classifying and identifying the I pig genetic origin and supplying molecular makers for conservation activities. Methods: This study sequenced the complete mitochondrial genome and used the sequencing result to analyze the phylogenetic relationship of I pig with Asian and European domestic pigs and wild boars. The full sequence was annotated and predicted the secondary tRNA. Results: The total length of I pig mitochondrial genome (accession number KX094894) was 16,731 base pairs, comprised two rRNA (12S and 16S), 22 tRNA and 13 mRNA genes. The annotation structures were not different from other pig breeds. Some component indexes as AT content, GC, and AT skew were counted, in which AT content (60.09%) was smaller than other pigs. We built the phylogenetic trees from full sequence and D loop sequence using Bayesian method. The result showed that I pig, Banna mini, wild boar (WB) Vietnam and WB Hainan or WB Korea, WB Japan were a cluster. They were a group within the Asian clade distinct from Chinese pigs and other Asian breeds in both phylogenetic trees (0.0004 and 0.0057, respectively). Conclusion: These results were similar to previous phylogenic study in Vietnamese pig and showed the genetic distinctness of I pig with other Asian domestic pigs.

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