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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.
Jeong, Lak Shin 이화여자대학교 세포신호전달연구센터 2007 고사리 세포신호전달 심포지움 Vol. No.9
S-Adenosylhomocysteine hydrolase catalyzes the hydrolysis of S-adenosylhomocysteine to adenosine and L-homocysteine. Inhibition of this enzyme accumulates S-adenosylhomocysteine, which in turn inhibits S-adenosyl-L-methionine dependent transmethylation, resulting in no formation of the capped methylated structure at the 5'-terminus of viral mRNA. Thus, S-adenosylhomocysteine hydrolase has been an attractive target for the development of broad spectrum of antiviral agents. Neplanocin A is a potent inhibitor of S-adenosylhomocysteine hydrolase. Neplanocin A inactivates the enzyme by depleting a cofactor(NAD^(+)) and its inhibition is reversed by incubation with with NAD^(+). Besides the cofactor depletion mechanism, we thought that neplanocin A can form a covalent bond with an active site of the enzyme in a Michael type reaction after the incubation with enzyme, but its irreversible action can be easily reversed by the presence of acidic 4'-hydrogen. Therefore, if we put the halogen atom into the C6 position of the neplanocin A, the resulting halo-neplanocin A anlogues might inhibit the enzyme irreversibly because of no acidic hydrogen at the 4'-position. As expected, fluoro-neplanocin A inhibited the enzyme irreversibly at the submicromolar concentration unlike neplanocin A showing the reversible inhibition. Synthesis and broad-spectrum of antiviral activity of the target compounds will be discussed in this symposium.
Jeong, Lak Shin,Yoo, Su Jeong,Lee, Kang Man,Koo, Mi Jeong,Choi, Won Jun,Kim, Hea Ok,Moon, Hyung Ryong,Lee, Min Young,Park, Jae Gyu,Lee, Sang Kook,Chun, Moon Woo 梨花女子大學校 藥學硏究所 2003 藥學硏究論文集 Vol.- No.12
Fluoroneplanocin A (12) was designed as a novel mechanism-based inhibitor of S-adenosylhomocysteine hydrolase (SAH) and efficiently synthesized via an electrophilic vinyl fluorination reaction (n-BuLi, N-fluorobenzenesulfonimide at -78℃). Fluoroneplanocin A exhibited 2-fold more potent SAH Inhibitory activity than the parent neplanocin A. A new mechanism of irreversible Inhibition discovered in this work might provide new alternatives in the design of a different class of antiviral agents operating via SAH inhibition.
Jeong, Lak Shin,Choe, Seung Ah,Gunaga, Prashantha,Kim, Hea Ok,Lee, Hyuk Woo,Lee, Sang Kook,Tosh, Dilip K.,Patel, Amit,Palaniappan, Krishnan K.,Gao, Zhan-Guo,Jacobson, Kenneth A.,Moon, Hyung Ryong 이화여자대학교 약학연구소 2008 藥學硏究論文集 Vol.- No.18
Truncated D-4'-thioadenosine derivatives lacking the 4'-hydroxymethylene moiety were synthesized starting from D-mannose, using cyclization to the 4-thiosugar and one-step conversion of the diol to the acetate as key steps At the human A₃ adenosine receptor (AR), N^(6)-substituted purine analogues bound potently and selectively and acted as antagonists in a cyclic AMP functional assay An N^(6)-(3-chlorobenzyl)purine analogue 9b displayed a K, value of 1 66 nM at the human A₃ AR Thus, truncated D-4'-thioadenosine is an excellent template for Ihe design of novel A₃ AR antagonists to act at both human and murine species.
Synthesis and Antiviral Activity of $2^1$-Fluorohexopyranosyl Nucleosides
Jeong, Lak-Shin,Lee, Jong-Eun,Kim, Hea-Ok,Chun, Moon-Woo The Pharmaceutical Society of Korea 1998 Archives of Pharmacal Research Vol.21 No.3
$2^1$-Fluorohexopyranosyl nucleosides 1a and 1b which contained a bioisosteric double bond and a fluorine were synthesized in 12 steps, starting from D-galactose. During diethylaminosulfur trifluoride (DAST) fluorination, retention of stereochemistry was observed through the participation of methoxy or chloro group at the 6-posiition of the purine base. The final nucleosides 1a and 1b were found to be inactive against HIV-1 and HSV-1,2.
Lak Shin, Jeong,Dilip K. Tosh,Won Jun, Choi,Sang Kook, Lee,You-Jin, Kang,Sun, Choi,Jin Hee, Lee,Hankil, Lee,Hyuk Woo, Lee,Hea Ok, Kim 이화여자대학교 약학연구소 2010 藥學硏究論文集 Vol.- No.20
The first synthesis of 2'-deoxy-2'-fluoro-4'-selenoarabinofuranosyl pyrimidines as potent anticancer agents was accomplished using the DAST fluorination as a key step. It was first revealed that selenium atom participated in the DAST fluorination of 4'-selenonucleosides and that conformational bias induced by bulky selenium acted as a decisive factor in the DAST fluorination. Among compounds tested, 2'-F-4'-seleno-ara-C (4a) exhibited highly potent anticancer activity in all cancer cell lines tested and was more potent than ara-C (1).
Jeong, Lak Shin,Moon, Hyung Ryong,Park, Jae Gyu,Shin, Dae Hong,Choi, Won Jun,Lee, Kang Man,Kim, Hea Ok,Chun, Moon Woo,Kim, Hee-Doo,Kim, Joong Hyup 梨花女子大學校 藥學硏究所 2003 藥學硏究論文集 Vol.- No.12
Halogenated analogues of neplanocin A were synthesized from the key intermediate 1, among which fluoro-neplanocin A was found to be novel mechanism-based irreversible inhibitor of S-Adenosylhomocysteine hydrolase.
Jeong, Lak Shin,Lee, Jeong A.,Moon, Hyung Ryong,Kim, Hea Ok,Lee, Kang Man,Lee, Hyun Joo,Chun, Moon Woo MARCEL DEKKER INC 2007 NUCLEOSIDES NUCLEOTIDES AND NUCLEIC ACIDS Vol.26 No.6-7
<P> Novel apio carbocyclic nucleosides 18-21 were asymmetrically synthesized as potential antiviral and antitumor agent, starting from D-ribose employing aldol reaction, RCM reaction and Mitsunobu reaction as key reactions.</P>
Synthesis And Anti-Hcv Activity Of 2''-&bgr;-Hydroxymethylated Nucleosides
Jeong, Lak Shin,Yoo, Byul Nae,Kim, Hea Ok,Lee, Kang Man,Moon, Hyung Ryong Taylor Francis 2007 Nucleosides, nucleotides & nucleic acids Vol.26 No.6
<P> Synthesis of 2' -&bgr;-hydroxymethyl nucleosides 3-6 was accomplished, using stereoselective hydroxymethylation as a key step. Adenine nucleoside 3 showed potent anti-HCV activity, implying that 2' -&bgr;-hydroxymethyl group has the appropriate electronic properties interfering with HCV polymerase.</P>