USE OF 2'-FLUORO-5-METHYL-BETA-L-ARABINOFURANOSYLURACIL AS A NOVEL ANTIVIRAL AGENT FOR HEPATITIS-B VIRUS AND EPSTEIN-BARR-VIRUS

被引:219
作者
CHU, CK
MA, TW
SHANHMUGANATHAN, K
WANG, CG
XIANG, YJ
PAI, SB
YAO, GQ
SOMMADOSSI, JP
CHENG, YC
机构
[1] YALE UNIV,SCH MED,DEPT PHARMACOL,NEW HAVEN,CT 06510
[2] UNIV ALABAMA,SCH MED,DEPT CLIN PHARMACOL,BIRMINGHAM,AL 35294
关键词
D O I
10.1128/AAC.39.4.979
中图分类号
Q93 [微生物学];
学科分类号
071005 ; 100705 ;
摘要
A novel anti-hepatitis B virus (anti-HBV) agent, 2'-fluoro-5-methyl-beta-L-arabinofuranosyluracil (L-FMAU), was synthesized and found to be a potent anti-HBV and anti-Epstein-Barr virus agent. Its in vitro potency was evaluated in 2.2.15 and H1 cells for anti-HBV and anti-Epstein-Barr virus activities, respectively. In vitro cytotoxicity in MT2, GEM, 2.2.15, and H1 cells was also assessed, and the results indicated high antiviral selectivities of L-FMAU in these cells.
引用
收藏
页码:979 / 981
页数:3
相关论文
共 28 条
[1]   SYNTHESIS OF ENANTIOMERICALLY PURE (2'R,5'S)-(-)-1-[2-(HYDROXYMETHYL)OXATHIOLAN-5-YL]CYTOSINE AS A POTENT ANTIVIRAL AGENT AGAINST HEPATITIS-B VIRUS (HBV) AND HUMAN-IMMUNODEFICIENCY-VIRUS (HIV) [J].
BEACH, JW ;
JEONG, LS ;
ALVES, AJ ;
POHL, D ;
KIM, HO ;
CHANG, CN ;
DOONG, SL ;
SCHINAZI, RF ;
CHENG, YC ;
CHU, CK .
JOURNAL OF ORGANIC CHEMISTRY, 1992, 57 (08) :2217-2219
[2]   A NOVEL CLASS OF 1,3-OXATHIOLANE NUCLEOSIDE ANALOGS HAVING POTENT ANTI-HIV ACTIVITY [J].
BELLEAU, B ;
BRASILI, L ;
CHAN, L ;
DIMARCO, MP ;
ZACHARIE, B ;
NGUYENBA, N ;
JENKINSON, HJ ;
COATES, JAV ;
CAMERON, JM .
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 1993, 3 (08) :1723-1728
[3]  
CHANG CN, 1992, J BIOL CHEM, V267, P13938
[4]  
CHEN CH, 1989, J BIOL CHEM, V264, P11934
[5]  
CHOU TC, 1987, ANTIMICROB AGENTS CH, V31, P355
[6]   THE SEPARATED ENANTIOMERS OF 2'-DEOXY-3'-THIACYTIDINE (BCH-189) BOTH INHIBIT HUMAN-IMMUNODEFICIENCY-VIRUS REPLICATION INVITRO [J].
COATES, JAV ;
CAMMACK, N ;
JENKINSON, HJ ;
MUTTON, IM ;
PEARSON, BA ;
STORER, R ;
CAMERON, JM ;
PENN, CR .
ANTIMICROBIAL AGENTS AND CHEMOTHERAPY, 1992, 36 (01) :202-205
[7]   EVALUATION OF THE POTENT ANTI-HEPATITIS-B VIRUS AGENT (-)CIS-5-FLUORO-1-[2-(HYDROXYMETHYL)-1,3-OXATHIOLAN-5-YL]CYTOSINE IN A NOVEL IN-VIVO MODEL [J].
CONDREAY, LD ;
JANSEN, RW ;
POWDRILL, TF ;
JOHNSON, LC ;
SELLESETH, DW ;
PAFF, MT ;
DALUGE, SM ;
PAINTER, GR ;
FURMAN, PA ;
ELLIS, MN ;
AVERETT, DR .
ANTIMICROBIAL AGENTS AND CHEMOTHERAPY, 1994, 38 (03) :616-619
[8]   INHIBITION OF THE REPLICATION OF HEPATITIS-B VIRUS INVITRO BY 2',3'-DIDEOXY-3'-THIACYTIDINE AND RELATED ANALOGS [J].
DOONG, SL ;
TSAI, CH ;
SCHINAZI, RF ;
LIOTTA, DC ;
CHENG, YC .
PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA, 1991, 88 (19) :8495-8499
[9]  
FRIED MW, 1992, HEPATOLOGY, V16, pA127
[10]   THE ANTI-HEPATITIS-B VIRUS ACTIVITIES, CYTOTOXICITIES, AND ANABOLIC PROFILES OF THE (-) AND (+) ENANTIOMERS OF CIS-5-FLUORO-1-[2-(HYDROXYMETHYL)-1,3-OXATHIOLAN-5-YL]CYTOSINE [J].
FURMAN, PA ;
DAVIS, M ;
LIOTTA, DC ;
PAFF, M ;
FRICK, LW ;
NELSON, DJ ;
DORNSIFE, RE ;
WURSTER, JA ;
WILSON, LJ ;
FYFE, JA ;
TUTTLE, JV ;
MILLER, WH ;
CONDREAY, L ;
AVERETT, DR ;
SCHINAZI, RF ;
PAINTER, GR .
ANTIMICROBIAL AGENTS AND CHEMOTHERAPY, 1992, 36 (12) :2686-2692